33 results on '"Mahama Ouattara"'
Search Results
2. 1-(2-Methylimidazo[1,2-a]pyridin-3-yl)-3,3-bis(methylsulfanyl)prop-2-enone monohydrate
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Yvon Bibila Mayaya Bisseyou, Drissa Sissouma, Severin D. Goulizan Bi, Mahama Ouattara, and R. C. A. Yao-Kakou
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Crystallography ,QD901-999 - Abstract
The title compound, C13H14N2OS2·H2O, appears in the form of bimolecular aggregate in which molecular components are linked by O—H...N hydrogen bonding. The nine-membered imidazo[1,2-a]pyridine system is almost planar, with a mean deviation of 0.026 (1) Å. An intramolecular C—H...O hydrogen bond forms within the imidazo[1,2-a]pyridine system. The crystal packing is consolidated by O—H...O and C—H...O hydrogen bonds, forming a supramolecular structure consisting of perpendicular infinite molecular chains running along the a and c axes.
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- 2009
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3. Pharmacotherapy of gastrointestinal strongylosis of small ruminants: An update
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Mahama Ouattara, Deto UJ-P N'guessan, and Songuigama Coulibaly
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Gastrointestinal strongylosis, which causes deadly seasonal diarrhea in small ruminants, is a major threat to the livestock population in sub-Saharan Africa. Moreover, livestock is a central component of food security. In addition to this threat, there is a poor veterinary coverage due to the increasing lack of effective anthelmintic drugs against strongyles because of the emergence and proliferation of chemo resistant strains. In this context, and given that the use of a vaccine is not widespread, the establishment of the therapeutic arsenal available to veterinarians to control strongyles will contribute to the food and economic security of rural populations. This review outlines the main pharmacochemical classes of anthelmintics used in the management of strongylosis of small ruminants.
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- 2022
4. MOLECULAR MODELING STUDIES OF BENZIMIDAZOLYL-CHALCONES AS ANTILEISHMANIAL AGENTS USING QSAR, DOCKING, ADME AND MOLECULAR DYNAMICS STUDIES
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Mahama Ouattara, Songuigama Coulibaly, Diomandé Sékou, Eunice Melissa Adouko, Abdulrahim Altoam Alzain, and Deto Ursul Jean- Paul N'guessan
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Introduction: Present leishmaniasis treatment regimen has many limitations including severe adverse effects, toxicity, and Leishmania strains resistance. In the present study, the objective is to perform QSAR, molecular docking and ADME prediction studies on benzimidazolylchalcones in order to select an antileishmanial drug candidate.Materials & methods: QSAR models were performed on 12 benzimidazolylchalcones with antileishmanial activities against promastigote strains of L. donovani. Binding free energy calculations were performed using MM-GBSA to assess the affinity of the ligands for the proteins. In addition, the three most active compounds (4a-c, IC50
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- 2022
5. Synthesis and Anticandidosic Activities of Some 3-Imidazo[1,2-a]Pyridinyl-1-Arylpropenone Derivatives
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Kouassi Francesco Adingra, Souleymane Coulibaly, Kacou Alain, Mahama Ouattara, and Drissa Sissouma
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Pharmacology (medical) - Published
- 2022
6. Discovery of 5-Chlorobenzimidazole-based as Promising Inhibitors of Chloroquine-Resistant Plasmodium Strains: Synthesis, Biological Evaluation, Molecular Docking and Computational Studies
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Songuigama Coulibaly, Abdulrahim A. Alzain, Drissa Sissouma, Mahama Ouattara, William Yavo, and Jean Paul N’Guessan
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Biochemistry ,biology ,Chloroquine ,Chemistry ,medicine ,biology.organism_classification ,Plasmodium ,medicine.drug ,Biological evaluation - Abstract
Background: To overcome drug resistance to current antimalarial drugs, we propose the synthesis and in vitro evaluation of the antiplasmodial activity of a series of 5-chlorobenzimidazolyl-chalcones against chloroquino sensitive (CQ-S) and chloroquino resistant (CQ-R) strains of P. falciparum. Objective: This study aimed to establish through structure-activity relationship studies and docking, the structural elements essential for antiplasmodial activities. Methods: The antiplasmodial activity of these benzimidazolylchalcones was carried out according to the Rieckmann microtest technique, followed by the determination of the concentrations inhibiting 50% of the production of parasitic HRP2 antigens (IC50) by ELISA. Chloroquine was used as a reference molecule with a sensitivity threshold set at 100 µM. Molecular docking was performed using sensitive (PDB ID: 1J3I) and resistant (PDB ID: 4DP3) dihydrofolate reductase-thymidylate synthase proteins (PfDHFR-TS). Results: All benzimidazolylchalcones tested expressed antiplasmodial activities especially against chloroquine resistant isolates (IC50 = 0.32-44.38 µM). The best profile against both isolates was the methoxylated derivative (3e) with an IC50 ranging from 0.32 to 1.96 µM. This compound had the best antimalarial activity against CQ-S isolates. On CQ-R isolates, the unsubstituted 5-chlorobenzimidazole derivative (3b) had exalted activity (IC50 = 0.78 µM). We selected a weakly active non-chlorinated derivative 3a and chlorinated derivatives 3b, 3d, 3e and 3f) with IC50< 3µM against the chloroquine-resistant strain to perform docking studies. These revealed that the pyrrolic nitrogen of benzimidazole and the ketone of propenone are the main chemical entities involved in the interaction at the receptor. Moreover, ADMET studies showed favorable pharmacokinetic properties. Conclusion: Molecular docking studies confirmed the experimental findings and revealed the possible interactions pattern. Derivatives 3b and 3e, which showed promising binding affinities against PfDHFR-TS, can be proposed as lead compounds for the development of antimalarial drug candidates.
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- 2021
7. New Biological Targets in Fungi and Novel Molecule under Development: A Review
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Songuigama Coulibaly, Amelanh S. Diakité, Jean-Paul Déto Ursul N'Guessan, Mahama Ouattara, Alain Kacou, Jean-Fabrice K. Koffi, and Tanguy K. A. Kouaho
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Biochemistry ,Antifungal drugs ,Molecule ,General Medicine ,Drug resistance ,Biology ,Mode of action - Abstract
Antifungal therapeutics is confronted today with the challenge of drug resistance of most fungal germs to current antifungal drugs. Faced with this situation, the search for new and more efficient antifungal molecules that avoid the phenomenon of drug resistance becomes an urgent task. The design of new antifungal drugs acting on new biological targets and/or by innovative mechanisms of action is essential in the fight against fungal infections. Current advances in molecular biology have identified new targets for the development of new antifungal therapy. Several biological targets for the development of new antifungal agents are currently being explored. Amongst these, the most promising are BET (Bromodomain and Extra-Terminal) proteins, Homoserine transacetylase (HTA), mannan cell wall, Glycosylphosphatidylinositols (GPI) anchor biosynthesis, Histone deacetylases, Sphingolipid biosynthesis, D9 fatty acid desaturase and Chitin biosynthesis. This review summarizes the new biological targets and their inhibitors under development as potential new antifungal drugs.
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- 2021
8. QSAR Study of a Serie of Benzimidazolylchalcone Derivatives by the Density Fonctional Theory (DFT) Method
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Ahmont Landry Claude Kablan, Jean Stéphane N’dri, Doumadé Zon, Drissa Sissouma, Mamadou Guy-Richard Koné, Adeyolé Timotou, and Mahama Ouattara
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Moment (mathematics) ,Dipole ,Quantitative structure–activity relationship ,Coefficient of determination ,Series (mathematics) ,Molecular descriptor ,Thermodynamics ,Quantum chemistry ,Standard deviation ,Mathematics - Abstract
This QSAR study involved a series of benzimidazolylchalcone derivatives. It allowed us to obtain a model from the molecular descriptors and anthelminthical activity against Haemonchus contortus. The molecular descriptors were obtained by applying the methods of quantum chemistry at the B3LYP/6-31G (d) level. The statistical indicators of the model are: the coefficient of determination R2 equals 0.990, the standard deviation S equals 0.209, the Fischer coefficient F equals 153.055 and the cross-validation coefficient equals 0.990. This model has good statistical performances. The quantum descriptors of dipole moment (μD) and electronic energy are responsible of the anthelminthic activity of benzimidazolylchalcone derivatives. In addition, the dipole moment is the priority descriptor for the prediction of the antibacterial activity of the studied compounds. The Eriksson et al. acceptance criteria used for the test set is verified. The values of the pCL100theo/pCL100exp ratio of the theoretical and experimental activities for the test set aim towards the unit.
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- 2021
9. Evaluation of Cytotoxic Profile of Some Chalcone Derivatives with Antimalarial Properties
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Mahama Ouattara, William Yavo, Marius Trésor Dable, Edgard Valery Adjogoua, Akissi Jeanne Koffi, Nkoua Badzi Cynthia, and Konan Dominique Tano
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Chalcone ,chemistry.chemical_compound ,biology ,Chemistry ,medicine ,Vero cell ,Cytotoxic T cell ,Plasmodium falciparum ,General Medicine ,medicine.disease ,biology.organism_classification ,Virology ,Malaria - Abstract
Malaria continues to kill thousands of people worldwide. People South of the Sahara are paying the heaviest price for this epidemic. In addition, the resistance of Plasmodium falciparum which spreads to artemisinin derivatives becomes worrying. To respond to this emergency, the search for new molecules effective against the parasite is essential. Otherwise, chalcones have shown their potential as an effective pharmaceutical agent in numerous studies. However, despite their mainly antiparasitic efficacy, several compounds have been shown to be cytotoxic. This study aimed to assess the cytotoxic profile of chalcone derivatives. Cytotoxicity tests were carried out according to the method described by Taylor and collaborators on Vero cells. The 96-well plates were used in carrying out this study, 100 µl of the compounds were added with concentrations ranging from 7.5 to 1000 µg/ml in DMEM. The results obtained report three compounds derivatives (Chal_B14, Chal_B17 & Chal_SCA03) no-cytotoxic with LDH product values between 129 - 132.5 U/L and ATP ranging from 8.55 to 13.6 RLU. The IC50s for no-cytotoxic compounds ranged from 102 to 236 µM. On the other hand, the cytotoxic compounds had IC50s of less than 30 µM. The results of this study show that the derivatives Chal_B14, Chal_B17 & Chal_SCA03 are candidate compounds with a view to finding new molecules.
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- 2020
10. Crystal structure, Hirshfeld surface analysis and contact enrichment ratios of 1-(2,7-dimethylimidazo[1,2-a]pyridin-3-yl)-2-(1,3-dithiolan-2-ylidene)ethanone monohydrate
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Abodou Jules Tenon, R. C. A. Yao-Kakou, Yvon Bibila Mayaya Bisseyou, Mahama Ouattara, and Pénétjiligué Adama Soro
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crystal structure ,Thio ,Crystal structure ,010403 inorganic & nuclear chemistry ,Ring (chemistry) ,01 natural sciences ,Research Communications ,lcsh:Chemistry ,Crystal ,chemistry.chemical_compound ,Pyridine ,Hirshfeld surface analysis ,Moiety ,General Materials Science ,hydrogen bond ,Hydrogen bond ,enrichment contact ,General Chemistry ,Condensed Matter Physics ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,Crystallography ,lcsh:QD1-999 ,chemistry ,hybrid molecule ,hybrid molecule ,Enone - Abstract
The synthesis of a hybrid molecule is reported. The crystal structure of the monohydrate was investigated using Hirshfeld surface analysis and enrichment contact ratios. Hydrogen bonds induced by guest water molecules are the main driving force in crystal packing formation., In the title hydrated hybrid compound C14H14N2OS2·H2O, the planar imidazo[1,2-a]pyridine ring system is linked to the 1,3-dithiolane moiety by an enone bridge. The atoms of the C—C bond in the 1,3-dithiolane ring are disordered over two positions with occupancies of 0.579 (14) and 0.421 (14) and both disordered rings adopt a half-chair conformation. The oxygen atom of the enone bridge is involved in a weak intramolecular C—H⋯O hydrogen bond, which generates an S(6) graph-set motif. In the crystal, the hybrid molecules are associated in R 2 2(14) dimeric units by weak C—H⋯O interactions. O—H⋯O hydrogen bonds link the water molecules, forming infinite self-assembled chains along the b-axis direction to which the dimers are connected via O—H⋯N hydrogen bonding. Analysis of intermolecular contacts using Hirshfeld surface analysis and contact enrichment ratio descriptors indicate that hydrogen bonds induced by water molecules are the main driving force in the crystal packing formation.
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- 2019
11. Ex vivo efficacy of selective chalcone derivatives on reference strains and field isolates ofPlasmodium falciparum
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Konan Dominique Tano, Eby Ignace Hervé Menan, Kigbafori Dieudonné Silue, Marius Trésor Dable, Mahama Ouattara, and William Yavo
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0301 basic medicine ,Chalcone ,biology ,Chemistry ,030231 tropical medicine ,030106 microbiology ,Public Health, Environmental and Occupational Health ,Plasmodium falciparum ,Context (language use) ,General Medicine ,biology.organism_classification ,Microbiology ,In vitro ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Infectious Diseases ,Parasitology ,Ex vivo - Abstract
The extension of Plasmodium falciparum resistance to existing antimalarial drugs is worrying. Faced with this problem, the search for new and effective molecules is necessary. In this context, six chalcone derivatives (B1, B11, B14, B17, SCA02 and SCA03) were tested on field isolates and then reference strains to evaluate their antiplasmodial activity by using the Rieckmann semi-microtest, recommended by WHO, for in vitro and ex vivo activity tests. Compounds B14 and B17 exhibited promising antiplasmodial activities (IC50s: 14.41-16.40 μM) regardless of the type of isolate. Compounds B1, B11, SCA02 and SCA03 showed a moderate inhibition of field isolates (IC50S: 25.63-48.29 μM) and very good activity against reference strains (IC50s: 3.82-10.03 μM). Therefore, more structural modulations should improve their efficiency and make these molecules very good candidates for future effective antimalarial drugs.
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- 2019
12. Design and structure-activity relationships anticandidosic of diazaheteroaryl functionalized by Michaël acceptors
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Jean-Paul N'Guessan Deto, Doumadé Zon, Drissa Sissouma, Mahama Ouattara, Mamidou Witabouna Kone, Aboudramane Kone, and Songuigama Coulibaly
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Benzimidazole ,chemistry.chemical_compound ,Imidazopyridine ,biology ,chemistry ,Michael reaction ,Context (language use) ,Candida albicans ,biology.organism_classification ,Combinatorial chemistry ,Chemical synthesis - Abstract
The management of candidiasis, once effective, is becoming more and more difficult with the increase of resistance of various Candida species to classical antifungals. It is in this context that we reported in our previous works the pharmacochemical development of new diazaheteroaryls derivatives functionalized with a Michael acceptor such as arylpropenone, arylacrylonitrile and arylcyanopropenone. These diazaheteroaryls derivatives with benzimidazolyl-arylpropenone or benzimidazolyl-arylacrylonitriles or benzimidazolyl-arylcyanopropenone and imidazopyridinyl-arylpropenones structure were obtained by chemical synthesis and then characterized by the usual spectroscopic methods (NMR and MS). The anticandidosic activities of these derivatives expressed as Minimum Inhibitory Quantity (MIQ) were determined in vitro on a clinical strain of Candida albicans, following the bioautography technique. The results show that diazaheteroaryls functionalized by a Michael acceptor have remarkable activities with IMQ ranging from 10 to 0.16 µg. Moreover, the anticandidosic performance of the different derivatives were related to the nature of the Michael acceptor and the structural variations undertaken on the benzene homocycle. This paper, which is the synthesis of a decade of research by our team, will address the pharmacochemical design, chemical synthesis and overall serial structure-anticandidosic activity studies of diaza-heteroaryls functionalized with a Michael acceptor in order to propose compounds that can be developed as anticandidosic drug candidates.
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- 2021
13. Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis
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Patrick Dallemagne, Mahama Ouattara, Cédric Lecoutey, Songuigama Coulibaly, Julien Briffotaux, Maria Virginia Buchieri, Christophe Rochais, Noelia Alonso-Rodriguez, Mena Cimino, Brigitte Gicquel, Damien Mornico, Centre d'Etudes et de Recherche sur le Médicament de Normandie (CERMN), Université de Caen Normandie (UNICAEN), Normandie Université (NU)-Normandie Université (NU), Université Félix Houphouët-Boigny (UFHB), Génétique mycobactérienne - Mycobacterial genetics, Institut Pasteur [Paris], Shenzhen Nanshan Center for Chronic Disease Control [Shenzhen, China] (ShenZhenCDC), Hub Bioinformatique et Biostatistique - Bioinformatics and Biostatistics HUB, Institut Pasteur [Paris]-Centre National de la Recherche Scientifique (CNRS), This work has received the financial support of the Service de Coopération et d’Action Culturelle of the French Embassy in Ivory Coast. This work was also supported by the European Seventh Framework Program Nanotherapeutics against Resistant Emerging Bacterial Patho-gens (NAREB Project 604237), as well as the Sanming Project of Medicine in Shenzhen (No. SZSM201603029). The analytical platform of CERMN is financially supported by Région Normandie and FEDER., European Project: 604237,EC:FP7:NMP,FP7-NMP-2013-LARGE-7,NAREB(2014), Institut Pasteur [Paris] (IP), and Institut Pasteur [Paris] (IP)-Centre National de la Recherche Scientifique (CNRS)
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Tuberculosis ,MESH: Mycobacterium tuberculosis ,medicine.drug_class ,[SDV]Life Sciences [q-bio] ,Antibiotics ,Mutant ,Antitubercular Agents ,Microbial Sensitivity Tests ,Quinolones ,MESH: Drug Design ,medicine.disease_cause ,01 natural sciences ,Microbiology ,Mycobacterium tuberculosis ,03 medical and health sciences ,Drug Resistance, Bacterial ,Drug Discovery ,MESH: Drug Resistance, Bacterial ,medicine ,MESH: Phenanthrolines ,030304 developmental biology ,Pharmacology ,0303 health sciences ,MESH: Microbial Sensitivity Tests ,MESH: Quinolones ,biology ,010405 organic chemistry ,Chemistry ,Organic Chemistry ,General Medicine ,medicine.disease ,biology.organism_classification ,MESH: Antitubercular Agents ,3. Good health ,0104 chemical sciences ,Dihydrophenanthrolinones ,Staphylococcus aureus ,Drug Design ,Antibacterial activity ,Rifampicin ,Bacteria ,Phenanthrolines ,medicine.drug ,Fluoroquinolones - Abstract
International audience; Several phenanthrolinic analogs of quinolones have been synthesized and their antibacterial activity tested against Mycobacterium tuberculosis, other mycobacterial species and bacteria from other genera. Some of them show high activity (of the range observed for rifampicin) against M. tuberculosis replicating in vitro and in vivo (infected macrophages) conditions. These derivatives show the same activity with all or several M. tuberculosis complex bacterial mutants resistant to fluoroquinolones (FQ). This opens the way to the construction of new drugs for the treatment of FQ resistant bacterial infections, including tuberculosis. Several compounds showed also activity against Staphylococcus aureus and probably other species. These compounds do not show major toxicity. We conclude that the novel phenanthrolinic derivatives described here are potent hits for further developments of new antibiotics against bacterial infectious diseases including tuberculosis in particular those resistant to FQ.
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- 2020
14. Ex vivo efficacy of selective chalcone derivatives on reference strains and field isolates of
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Marius Trésor, Dable, Konan Dominique, Tano, Mahama, Ouattara, Kigbafori Dieudonné, Silue, Eby I Hervé, Menan, and William, Yavo
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Antimalarials ,Inhibitory Concentration 50 ,Chalcone ,Plasmodium falciparum ,Animals ,Article - Abstract
The extension of Plasmodium falciparum resistance to existing antimalarial drugs is worrying. Faced with this problem, the search for new and effective molecules is necessary. In this context, six chalcone derivatives (B1, B11, B14, B17, SCA02 and SCA03) were tested on field isolates and then reference strains to evaluate their antiplasmodial activity by using the Rieckmann semi-microtest, recommended by WHO, for in vitro and ex vivo activity tests. Compounds B14 and B17 exhibited promising antiplasmodial activities (IC(50s): 14.41–16.40 μM) regardless of the type of isolate. Compounds B1, B11, SCA02 and SCA03 showed a moderate inhibition of field isolates (IC(50S): 25.63–48.29 μM) and very good activity against reference strains (IC50s: 3.82–10.03 μM). Therefore, more structural modulations should improve their efficiency and make these molecules very good candidates for future effective antimalarial drugs.
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- 2020
15. Pharmacochemical Aspects of the Evolution from Erythromycin to Neomacrolides, Ketolides and Neoketolides
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Mahama, Ouattara, primary, Songuigama, Coulibaly, additional, and Jean-Paul, N’Guessan Deto, additional
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- 2020
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16. Anticancer Activities and QSAR Study of Novel Agents with a Chemical Profile of Benzimidazolyl-Retrochalcone
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Mahama, Ouattara, primary, Aboudramane, Koné, additional, Soleymane, Koné, additional, Sylvain, Collet, additional, Sekou, Diomandé, additional, and Drissa, Sissouma, additional
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- 2020
- Full Text
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17. Composés á structure imidazopyridinyl-arylpropénone, nouveaux agents anti-infectieux potentiels
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Mamidou W. Kone, Drissa Sissouma, Mahama Ouattara, and William Yavo
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0301 basic medicine ,03 medical and health sciences ,030104 developmental biology ,010405 organic chemistry ,General Chemical Engineering ,General Chemistry ,01 natural sciences ,0104 chemical sciences - Abstract
Resume Le present travail decrit la conception, par juxtaposition d’entites anti-infectieuses, d’une serie de composes hybrides a structure imidazopyridinyl-arylpropenone. Ces composes ( 5a–y) ont ete synthetises par crotonisation entre la 1-(2-methylimidazo[1,2- a ]pyridin-3-yl)ethanone ( 3 ) et divers benzaldehydes ( 4 ). Leurs structures ont ete determinees par spectrometrie de masse RMN et ESI. Le criblage de ces composes vis-a-vis d’agents pathogenes parasitaires et microbiens montre que le compose 5q (CI 50 = 1,52 μM) pourrait etre retenu pour un developpement contre le paludisme a Plasmodium falciparum chloroquino-resistant. Contre les helminthoses veterinaires a Haemonchus contortus , trois composes s’averent d'interet : il s’agit des composes 5n, 5s et 5w (CL 100 = 7,1–1,5 nM). Contre les candidoses a Candida albicans pharmacoresistants, trois autres composes meritent d’etre retenus : les composes 5e, 5g et 5v (QMI = 1,25–0,31 μg). Cette etude montre que l’enchainement fonctionnel arylpropenone vectorise par l’imidazopyridine peut etre considere comme un nouveau pharmacophore d’activites anti-infectieuses potentielles.
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- 2016
18. Analgesic and anti-inflammatory properties of synthesized imidazopyrinidyl-chalcones: Relationship activity and structure
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Landry, Kouakou Sylvain, Mahama, Ouattara, Songuigama, Coulibaly, Jean Paul, Nguessan, Genevieve, Irie-N'Guessan Amenan, Gisele, Kouakou-Siransy, Landry, Kouakou Sylvain, Mahama, Ouattara, Songuigama, Coulibaly, Jean Paul, Nguessan, Genevieve, Irie-N'Guessan Amenan, and Gisele, Kouakou-Siransy
- Abstract
Background : The effective management of pain in clinic is still challenging practitioner because of the many side effects associated with the use of current drugs, which can even affect life quality of the patients. Chalcones are described as compounds that have various pharmacological activities such as antioxidants, anti-inflammatories, anticancer antifungals and antibacterials. The objective of this study was to evaluate the analgesic and anti-inflammatory properties of two (2) synthesized imidazopyridinyl-chalcones. Materials and Methods : Imidazopyridinyl-chalcones tested V1 and V2, different by the substituent, type hydroxyl group for V1 and diethylamine for V2, were synthesized by the Department of Organic and Therapeutic Chemistry of Pharmaceutical and Biological Sciences (Cote d'Ivoire). The analgesic and anti-inflammatory activities were performed in mice and rats respectively by acetic acid-induced writhes test according to the method described by Koster et al and formalin-induced irritation test performed by Dubuisson et al . Results : V1 and V2 showed inhibition of contortions induced by acid acetic 1%, with greater analgesic effect for V2 at lower doses, while the opposite was observed for V1. At concentration of 3.125 mg/kg b. wt., V2 was 77.78% and V1 reach this percentage around 72.22% at 50 mg/kg b.wt., whereas that of paracetamol 100 mg/kg b. wt., used as a reference was about 48%. The anti-inflammatory effect of V2 (43.51%) was also higher compared to V1 (34.85%) at 3.125 mg/kg b.wt, but when doses increases at 12.25 mg/kg b. wt., the effect was non-significantly different to that of ketoprofen (69.98%) at 10 mg/kg b. wt., and range 48.57% and 47.73% respectively for V2 and V1. Conclusion : Imidazopyridinyl-chalcones is a good model for the development of new molecules and it would appear that the presence of electron donor group like diethylamine is better than hydroxyl to push up analgesic and/or anti-inflammatory activities.
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- 2018
19. Discovery of imidazo[1,2-a]pyridine-based anthelmintic targeting cholinergic receptors of Haemonchus Contortus
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Cécile Enguehard-Gueiffier, Claude L. Charvet, Cedric Neveu, Pierre-Olivier Delaye, Jean-Paul Déto Ursul N'Guessan, Hassan Allouchi, Mahama Ouattara, Mélanie Pénichon, Alain Gueiffier, Infectiologie et Santé Publique (UMR ISP), Institut National de la Recherche Agronomique (INRA)-Université de Tours (UT), Université Félix Houphouët-Boigny (UFHB), Institut National de la Santé et de la Recherche Médicale (INSERM), SCAC department of embassy of France in Abidjan, Ivory Coast, and Institut National de la Recherche Agronomique (INRA)-Université de Tours
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0301 basic medicine ,Pyridines ,Clinical Biochemistry ,Pharmaceutical Science ,Pharmacology ,01 natural sciences ,Biochemistry ,Parasitic Sensitivity Tests ,Haemonchus contortus ,Drug Discovery ,Anthelmintic ,Receptors, Cholinergic ,Imidazo[1 ,2-a]pyridine ,Cholinergic receptors ,Antagonist effect ,Anthelmintics ,biology ,Molecular Structure ,Drug discovery ,Chemistry ,Microbiology and Parasitology ,Microbiologie et Parasitologie ,3. Good health ,[SDV.MP]Life Sciences [q-bio]/Microbiology and Parasitology ,Molecular Medicine ,Haemonchus ,medicine.symptom ,medicine.drug ,pharmacologie ,parasite animal ,03 medical and health sciences ,Structure-Activity Relationship ,parasitic diseases ,medicine ,Structure–activity relationship ,Animals ,Mode of action ,Molecular Biology ,Dose-Response Relationship, Drug ,anthelminthique ,Organic Chemistry ,Antagonist ,biology.organism_classification ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,030104 developmental biology ,Mechanism of action ,Cholinergic - Abstract
We report the synthesis of a series of imidazo[1,2- a ]pyridine-based molecules as anthelmintic against the livestock parasite Haemonchus contortus . The molecules were tested by using Larval Paralysis Test (LPT), in order to target ionic channels, as most of the prominent marketed anthelminthics present such mechanism of action. The most active compound ( 5e ) displayed paralysis on H. contortus stage 3 larvae until 31.25 µM. Effect of 5e on H. contortus cholinergic receptors (L-AChR1 and 2) was characterized via electrophysiological measurement and a rare antagonist mode of action was unveiled.
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- 2017
20. DESIGN AND PHARMACOCHEMICAL DEVELOPMENT OF NEW ANTHELMINTICS WITH BENZIMIDAZOLYL ARYLPROPENONE PROFILE: STRUCTURE-ACTIVITY RELATIONSHIP.
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Mahama, Ouattara, Jean-Paul, N'Guessan Deto, Songuigama, Coulibaly, Drissa, Sissouma, and Mamidou, Koné W.
- Abstract
On the basis of our previous study, which had demonstrated the strong anthelmintic potential of benzimidazole-2-arylpropenones, we proposed to extend the anthelmintic evaluation by testing anovel series of benzimidazole against Haemonchus contortus. The aimof this work is to appreciate the impact of the bioisoteric replacement of arylpropenone by arylacrylonitrile. Furthermore, we have established the structural elements necessary to get good anthelmintic activities in series of 2-substituted benzimidazoles. The structure-activity relationship studies made after all biological evaluations gathered, revealed that in series benzimidazolyl-phenylpropenones, excellent anthelmintic activities similar to those of Ivermectin have been achieved with the unsubstituted phenyl derivative, with the metahydroxyphenyl derivative, and by replacing the benzene homocycle with a heterocycle like pyridine or furan. Of all the variations made around the benzimidazole heterocycle, it appears that the introduction of a chlorine atom on one of the potential sites of metabolism of benzimidazole (C-5), coupled with the non-substitution of pyrrolic nitrogen, is favorable for obtaining powerful anthelminthic activities superior to those of Ivermectin and similar to those of fenbendazole. The isosteres of the arylpropenone chain, namely arylacrylonitrile and aryl-a-cyanopropenone or even its cyclized derivative (arylcyclohexenone), did not allow the enhancement of anthelmintic activities expected. [ABSTRACT FROM AUTHOR]
- Published
- 2020
21. Choc électrique externe à Abidjan : bilan de dix ans de pratique à l’Institut de Cardiologie d’Abidjan, Côte d’Ivoire
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Mahama Ouattara, Anicet Adoubi, Djenamba Bamba-Kamagate, J. B. Anzouan-Kacou, Joseph Kouadio Kouame, Evelyne Ake-Traboulsy, Marie-Paule N’Cho-Motto, Iklo Coulibaly, Kouao Christophe Konin, Fatoumata Traore, and Roland N'Guetta
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Gynecology ,medicine.medical_specialty ,business.industry ,Direct current cardioversion ,Medicine ,Pharmacology (medical) ,business - Abstract
Resume La cardioversion electrique externe est efficace dans le traitement des arythmies. Peu de travaux lui ont ete consacres a Abidjan. Ce travail avait pour objectif de faire le bilan de 10 ans de pratique. Methode Mille trois cent quatrevingt-onze dossiers d’arythmies ont ete retrospectivement analyses. Resultats Cent deux patients ont ete choques ; 181 chocs delivres avec une energie moyenne de 262,1 Joules (J). La procedure a ete efficace chez 84 patients (82,3 %). Elle a echoue chez 18 patients (17,7 %). Huit complications graves ont ete enregistrees comprenant 1 dysfonction sinusale, 1 œdeme aigu du poumon, 1 metrorragie, 2 accidents vasculaires cerebraux et 1 embolie pulmonaire. Deux deces ont ete releves ; l’un pour tachycardie ventriculaire postoperatoire, l’autre pour tachycardie ventriculaire sur insuffisance cardiaque terminale. Conclusion Le choc electrique externe est efficace et sur. Les complications sont le plus souvent le fait des conditions cliniques plutot que de la procedure.
- Published
- 2011
22. Exploration of potential prodrug approach of the bis-thiazolium salts T3 and T4 for orally delivered antimalarials
- Author
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Michel Boisbrun, Henri Vial, Suzanne Peyrottes, Karine Alarcon, Michèle Calas, Xavier J. Salom-Roig, Marjorie Maynadier, Mahama Ouattara, Sergio A. Caldarelli, Sharon Wein, Alain Pellet, and Abdallah Hamze
- Subjects
Plasmodium ,Plasmodium vinckei ,Clinical Biochemistry ,Pharmaceutical Science ,Pharmacology ,Biochemistry ,Chemical synthesis ,Antimalarials ,Mice ,Structure-Activity Relationship ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Parasitic Sensitivity Tests ,Oral administration ,parasitic diseases ,Drug Discovery ,Animals ,Structure–activity relationship ,Prodrugs ,Molecular Biology ,030304 developmental biology ,0303 health sciences ,Dose-Response Relationship, Drug ,Molecular Structure ,biology ,Chemistry ,Organic Chemistry ,Stereoisomerism ,Plasmodium falciparum ,Prodrug ,biology.organism_classification ,Malaria ,3. Good health ,Thiocarbamate ,Thiazoles ,030220 oncology & carcinogenesis ,Molecular Medicine ,Salts ,Thiocarbonate - Abstract
We report here the synthesis and biological evaluation of a series of 37 compounds as precursors of potent antimalarial bis-thiazolium salts (T3 and T4). These prodrugs were either thioester, thiocarbonate or thiocarbamate type and were synthesized in one step by reaction of an alkaline solution of the parent drug with the appropriate activated acyl group. Structural variations affecting physicochemical properties were made in order to improve oral activity. Twenty-five of them exhibited potent antimalarial activity with IC(50) lower than 7nM against Plasmodium falciparum in vitro. Notably, 3 and 22 showed IC(50)=2.2 and 1.8nM, respectively. After oral administration 22 was the most potent compound clearing the parasitemia in Plasmodium vinckei infected mice with a dose of 1.3mg/kg.
- Published
- 2010
23. Synthesis and in vitro antifungal evaluation of 2-thioalkylaryl-benzimidazoles derivatives against Candida albicans
- Author
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Drissa Sissouma, Venance Martial Say, Mamidou Witabouna Kone, Mahama Ouattara, Sagne Jacques Akpa, Ané Adjou, and Roger Simplice Pépin Zoakouma
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Antifungal ,Benzimidazole ,biology ,010405 organic chemistry ,medicine.drug_class ,Stereochemistry ,010402 general chemistry ,biology.organism_classification ,01 natural sciences ,In vitro ,0104 chemical sciences ,chemistry.chemical_compound ,chemistry ,medicine ,Nitro ,Reactivity (chemistry) ,Candida albicans - Abstract
The aim of this study is to find potent biomolecules against infectious germs. Based on the reactivity of some key positions of the benzimidazole core, the first part of this work consisted of the synthesis of a series of substituted 2-thioalkylaryl-benzimidazoles 3a-d. Then, another series of N -alkyl-2-thioalkylarylbenzimidazoles 5a-d, 7a-c and 9b-c was also prepared from 2-thioalkylaryl-benzimidazoles by substitution on position-1 of benzimidazole core using the corresponding functionalized ethyl. The chemical structures of these compounds are determined by NMR ( 1 H, 13 C) and mass spectrometry. The second part concerned the in vitro antifungal activity evaluation of some of the synthesized compounds on Candida albicans . According to the results of evaluation, four compounds (3b, 3c, 3d and 9c) of the substituted 2-thioalkylaryl-benzimidazoles prove to be potent antifungal agent. Introduction of nitro group (NO 2 ) increased significantly the antifungal activity so that their IMQ is ranging between 0.03 and 0.008 μg (or 333 to 1250 times more efficient than the ketoconazole’s). Keywords : synthesis of 2-thioalkylaryl-benzimidazole, antifungal activity, candida albicans.
- Published
- 2016
24. Disulfide prodrugs of albitiazolium (T3/SAR97276): synthesis and biological activities
- Author
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Mahama Ouattara, Michèle Calas, Marjorie Maynadier, Matthieu Hamel, Christian Périgaud, Jean-Frédéric Duckert, Sergio A. Caldarelli, Sharon Wein, Alain Pellet, Suzanne Peyrottes, Henri Vial, Institut des Biomolécules Max Mousseron [Pôle Chimie Balard] (IBMM), Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)-Université de Montpellier (UM)-Ecole Nationale Supérieure de Chimie de Montpellier (ENSCM), Dynamique des interactions membranaires normales et pathologiques (DIMNP), Université Montpellier 1 (UM1)-Université Montpellier 2 - Sciences et Techniques (UM2)-Université de Montpellier (UM)-Centre National de la Recherche Scientifique (CNRS), Sanofi Research & Development, and Sanofi Recherche & Development
- Subjects
Stereochemistry ,Lysine ,Plasmodium falciparum ,Stereoisomerism ,010402 general chemistry ,01 natural sciences ,chemistry.chemical_compound ,Antimalarials ,Mice ,Structure-Activity Relationship ,Valine ,Bromide ,Oral administration ,Drug Discovery ,Structure–activity relationship ,Animals ,Prodrugs ,Disulfides ,chemistry.chemical_classification ,010405 organic chemistry ,[CHIM.ORGA]Chemical Sciences/Organic chemistry ,Prodrug ,0104 chemical sciences ,3. Good health ,Malaria ,Thiazoles ,Enzyme ,chemistry ,Molecular Medicine - Abstract
International audience; We report herein the design, synthesis, and biological screening of a series of 15 disulfide prodrugs as precursors of albitiazolium bromide (T3/SAR97276, compound 1), a choline analogue which is currently being evaluated in clinical trials (phase II) for severe malaria. The corresponding prodrugs are expected to revert back to the active bis-thiazolium salt through an enzymatic reduction of the disulfide bond. To enhance aqueous solubility of these prodrugs, an amino acid residue (valine or lysine) or a phosphate group was introduced on the thiazolium side chain. Most of the novel derivatives exhibited potent in vitro antimalarial activity against P. falciparum. After oral administration, the cyclic disulfide prodrug 8 showed the best improvement of oral efficacy in comparison to the parent drug.
- Published
- 2012
25. Synthesis and in vitro nematicidal activity of new chalcones vectorised by imidazopyridine
- Author
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Herve E. Menan, Mahama Ouattara, Drissa Sissouma, Lassina Ouattara, Ane Adjou, and Mamidou W. Kone
- Subjects
Pharmacology ,Imidazopyridine ,Chalcone ,chemistry.chemical_compound ,Chemistry ,Stereochemistry ,Pharmaceutical Science ,Organic chemistry ,Carbon-13 NMR ,In vitro - Abstract
A series of 3-(3-Arylpropenoyl)imidazopyridine (5a to z) was synthesized by crotonization reaction of 2-methyl-3-acetylimidazopyridine with arylaldehyde derivatives. Structuraldetermination of these new chalcones was done by 1H nuclear magnetic resonance (NMR),13C NMR and electrospray ionization (ESI) mass spectroscopy. All compounds have beenevaluated in vitro for their anthelmintic activities against Haemonchus contortus. Compounds5n, 5s, 5t and 5w showed a great nematicidal activity (LC100) ranging between 0.0005 and0.002 µg/ml. The activity of these four chalcones was equivalent to that of fenbendazole andivermectin which were reference anthelmintic drugs. This study has shown that imidazopyridine-chalcone derivatives are promising candidates for the development of new anthelmintic agents. Key words: Haemonchus contortus, imidazopyridine, chalcone, nematicidal activity.
- Published
- 2011
26. [Not Available]
- Author
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Iklo, Coulibaly, Kouao Christophe, Konin, Anicet, Adoubi, Joseph Kouadio, Kouame, Fatoumata, Traore, Djénamba, Bamba-Kamagaté, Roland Aka, N'Guetta, Marie-Paule, N'Cho-Motto, Mahama, Ouattara, Jean-Baptiste, Anzouan-Kacou, and Evelyne, Ake-Traboulsy
- Abstract
Direct current cardioversion is effective in arrhythmias' termination. Few is known about its use in our practice. This work aims to report its outcomes over a ten-year period in Abidjan.One thousand, three hundred and ninety one charts of arrhythmic patients were reviewed.Cardioversion was attempted in 102 patients. One hundred and eighty one shocks were delivered with a mean energy of 262, 1 joules. Success occurred in 84 patients (82,3%). Cardioversion failed in 18 patients mostly in atrial fibrillation. Eight serious complications (7,8%) occurred including 1 sinus node dysfunction, 1 pulmonary oedema, 1 metrorrhagia, 2 stroke, 1 pulmonary embolism. Two patients with ventricular tachycardia died of end-stage heart failure and aftermath of a mitral valve surgery.Direct current cardioversion is effective and safe in our practice. Complications are predominantly due to the medical environment such as antiarrhythmic drugs use or clinical conditions.
- Published
- 2011
27. [Direct current cardioversion in Abidjan: report of a ten-year practice in Institute of Cardiology of Abidjan, Ivory Coast]
- Author
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Iklo, Coulibaly, Kouao Christophe, Konin, Anicet, Adoubi, Joseph Kouadio, Kouame, Fatoumata, Traore, Djénamba, Bamba-Kamagaté, Roland, Aka N'guetta, Marie-Paule, N'cho-Motto, Mahama, Ouattara, Jean-Baptiste, Anzouan-Kacou, and Evelyne, Ake-Traboulsy
- Subjects
Male ,Cote d'Ivoire ,Treatment Outcome ,Atrial Fibrillation ,Electric Countershock ,Humans ,Arrhythmias, Cardiac ,Female ,Middle Aged ,Aged - Abstract
Direct current cardioversion is effective in arrhythmias' termination. Few is known about its use in our practice. This work aims to report its outcomes over a ten-year period in Abidjan.One thousand, three hundred and ninety one charts of arrhythmic patients were reviewed.Cardioversion was attempted in 102 patients. One hundred and eighty one shocks were delivered with a mean energy of 262, 1 joules. Success occurred in 84 patients (82,3%). Cardioversion failed in 18 patients mostly in atrial fibrillation. Eight serious complications (7,8%) occurred including 1 sinus node dysfunction, 1 pulmonary oedema, 1 metrorrhagia, 2 stroke, 1 pulmonary embolism. Two patients with ventricular tachycardia died of end-stage heart failure and aftermath of a mitral valve surgery.Direct current cardioversion is effective and safe in our practice. Complications are predominantly due to the medical environment such as antiarrhythmic drugs use or clinical conditions.
- Published
- 2011
28. Synthesis and antifungal activities of some benzimidazolyl-chalcones, analogues of chlormidazole
- Author
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Drissa, Sissouma, primary, Mahama, Ouattara, additional, and Mamidou, W Kone, additional
- Published
- 2015
- Full Text
- View/download PDF
29. Design and synthesis of amidoxime derivatives for orally potent C-alkylamidine-based antimalarial agents
- Author
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Sharon Wein, Henri Vial, Mahama Ouattara, Thierry Durand, Stéphanie Ortial, Séverine Denoyelle, Roger Escale, Yen Vo-Hoang, Institut des Biomolécules Max Mousseron [Pôle Chimie Balard] (IBMM), Ecole Nationale Supérieure de Chimie de Montpellier (ENSCM)-Institut de Chimie du CNRS (INC)-Université de Montpellier (UM)-Centre National de la Recherche Scientifique (CNRS), Université de Montpellier (UM), Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université de Montpellier (UM)-Ecole Nationale Supérieure de Chimie de Montpellier (ENSCM), Dynamique des interactions membranaires normales et pathologiques (DIMNP), Université Montpellier 1 (UM1)-Université Montpellier 2 - Sciences et Techniques (UM2)-Université de Montpellier (UM)-Centre National de la Recherche Scientifique (CNRS), Europe, and European Project: LSHP-CT-2005-018834
- Subjects
Stereochemistry ,Chemistry, Pharmaceutical ,Clinical Biochemistry ,Plasmodium falciparum ,Design of prodrug ,Pharmaceutical Science ,Administration, Oral ,[CHIM.THER]Chemical Sciences/Medicinal Chemistry ,Parasitemia ,Pharmacology ,Biochemistry ,Chemical synthesis ,Antioxidants ,Specific O-substitutions ,Antiprotozoal Agent ,Antimalarials ,Mice ,In vivo ,Oral administration ,Alkylamidoxime ,Drug Discovery ,Oral antimalarial agent ,medicine ,[CHIM]Chemical Sciences ,Animals ,Humans ,Prodrugs ,Clearance of parasitemia ,Antimalarial Agent ,Molecular Biology ,C-Alkylamidine ,biology ,Dose-Response Relationship, Drug ,[CHIM.ORGA]Chemical Sciences/Organic chemistry ,Chemistry ,Organic Chemistry ,Prodrug ,biology.organism_classification ,medicine.disease ,Malaria ,Models, Chemical ,Drug Design ,Molecular Medicine - Abstract
International audience; Within the frame of the design of prodrug candidates to deliver a C-alkylamidine antimalarial agent, we showed that specific O-substitutions were needed on the alkylamidoxime structure. Among the newly synthesized molecules, bis-oxadiazolone and bis-O-methylsulfonylamidoxime derivatives induced a complete clearance of parasitemia in mice after oral administration.
- Published
- 2008
30. Potent antimalarial activity of 2-aminopyridinium salts, amidines, and guanidines
- Author
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Gilles Piquet, Michèle Calas, Marie-Laure Ancelin, Yann Bordat, Mahama Ouattara, Zyta M. Ziora, Roger Escale, Henri Vial, Laboratoire des Amino-acides Peptides et Protéines (LAPP), Centre National de la Recherche Scientifique (CNRS)-Université Montpellier 2 - Sciences et Techniques (UM2)-Université Montpellier 1 (UM1), Institut des Biomolécules Max Mousseron [Pôle Chimie Balard] (IBMM), Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)-Université de Montpellier (UM)-Ecole Nationale Supérieure de Chimie de Montpellier (ENSCM), Université Montpellier 1 (UM1), Laboratoire de Chimie Thérapeutique et Synthèse de Médicaments (LCTSM), Université d'Abidjan-Cocody, Laboratoire de Chimie Thérapeutique et Synthèse de Médicaments, Dynamique moléculaire des interactions membranaires (DMIM), Centre National de la Recherche Scientifique (CNRS)-Université Montpellier 2 - Sciences et Techniques (UM2), Dynamique des interactions membranaires normales et pathologiques (DIMNP), Centre National de la Recherche Scientifique (CNRS)-Université de Montpellier (UM)-Université Montpellier 2 - Sciences et Techniques (UM2)-Université Montpellier 1 (UM1), Pathologies du système nerveux : recherche épidémiologique et clinique, Université Montpellier 1 (UM1)-IFR76-Institut National de la Santé et de la Recherche Médicale (INSERM), Neuropsychiatrie : recherche épidémiologique et clinique (PSNREC), Université Montpellier 1 (UM1)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Université de Montpellier (UM), Chimie biomoléculaire et des interactions biologiques (CBIB), and Centre National de la Recherche Scientifique (CNRS)-Université Montpellier 1 (UM1)
- Subjects
Stereochemistry ,Plasmodium falciparum ,Amidines ,Aminopyridines ,Pyridinium Compounds ,010402 general chemistry ,Guanidines ,01 natural sciences ,Chemical synthesis ,Amidine ,Antimalarials ,Structure-Activity Relationship ,chemistry.chemical_compound ,MESH: Amidines ,MESH: Quaternary Ammonium Compounds ,MESH: Structure-Activity Relationship ,Drug Discovery ,Animals ,Ammonium ,MESH: Animals ,[SDV.BBM]Life Sciences [q-bio]/Biochemistry, Molecular Biology ,Methylene ,Alkyl ,MESH: Plasmodium falciparum ,chemistry.chemical_classification ,010405 organic chemistry ,Cationic polymerization ,MESH: Antimalarials ,0104 chemical sciences ,3. Good health ,MESH: Aminopyridines ,Quaternary Ammonium Compounds ,MESH: Guanidines ,chemistry ,MESH: Pyridinium Compounds ,Molecular Medicine ,Amine gas treating ,Aliphatic compound - Abstract
We describe the design, synthesis, and antimalarial activity of 60 bis-tertiary amine, bis-2(1 H)-imino-heterocycle, bis-amidine, and bis-guanidine series. Bis-tertiary amines with a linker from 12 to 16 methylene groups were active against the in vitro growth of Plasmodium falciparum within the 10 (-6)-10 (-7) M concentration range. IC 50 decreased by 2 orders of magnitude for bis-2-aminopyridinium salts, bis-amidines, and bis-guanidines (27 compounds with IC 50 < 10 nM). Increasing the alkyl chain length from 6 to 12 methylene groups led to increased activity, while beyond this antimalarial activity decreased. Antimalarial activities appear to be strictly related to the basicity of the cationic head with an optimal p K a over 12.5. Maximal activity occurs for bis-2-aminopyridinium, two C-duplicated bis-amidines, and three bis-guanidines, with IC 50 values lower than 1 nM. In comparison to similar quaternary ammonium salts, amidinium compounds have distinct structural requirements for antimalarial activity and likely additional binding opportunities on account of their hydrogen-bond-forming properties.
- Published
- 2007
31. Synthesis and antimalarial activity of new 1,12-bis(N,N'-acetamidinyl)dodecane derivatives
- Author
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Michèle Calas, Sharon Wein, Yen Vo Hoang, Roger Escale, Mahama Ouattara, Henri Vial, Université Montpellier 1 (UM1), Laboratoire de Chimie Thérapeutique et Synthèse de Médicaments (LCTSM), Université d'Abidjan-Cocody, Dynamique des interactions membranaires normales et pathologiques (DIMNP), Université Montpellier 1 (UM1)-Université Montpellier 2 - Sciences et Techniques (UM2)-Université de Montpellier (UM)-Centre National de la Recherche Scientifique (CNRS), Centre d'études sur la cooperation juridique internationale (CECOJI), Université de Poitiers-Centre National de la Recherche Scientifique (CNRS), Laboratoire des Amino-acides Peptides et Protéines (LAPP), Université Montpellier 1 (UM1)-Université Montpellier 2 - Sciences et Techniques (UM2)-Centre National de la Recherche Scientifique (CNRS), and Centre National de la Recherche Scientifique (CNRS)-Université de Montpellier (UM)-Université Montpellier 2 - Sciences et Techniques (UM2)-Université Montpellier 1 (UM1)
- Subjects
MESH: Plasmodium cynomolgi ,Clinical Biochemistry ,Amidines ,Pharmaceutical Science ,Administration, Oral ,01 natural sciences ,Biochemistry ,Chemical synthesis ,chemistry.chemical_compound ,Mice ,Oral administration ,Drug Discovery ,MESH: Animals ,Antimalarial Agent ,Malaria, Falciparum ,MESH: Plasmodium falciparum ,0303 health sciences ,MESH: Malaria, Falciparum ,MESH: Indicators and Reagents ,Biological activity ,Prodrug ,3. Good health ,MESH: Administration, Oral ,Molecular Medicine ,Female ,Injections, Intraperitoneal ,MESH: Injections, Intraperitoneal ,Plasmodium cynomolgi ,Stereochemistry ,Dodecane ,Plasmodium falciparum ,MESH: Malaria ,MESH: Hydroxylation ,Hydroxylation ,03 medical and health sciences ,Antimalarials ,MESH: Amidines ,In vivo ,Alkanes ,Animals ,Humans ,[SDV.BBM]Life Sciences [q-bio]/Biochemistry, Molecular Biology ,Molecular Biology ,MESH: Mice ,030304 developmental biology ,MESH: Humans ,010405 organic chemistry ,Organic Chemistry ,MESH: Antimalarials ,In vitro ,0104 chemical sciences ,Malaria ,MESH: Alkanes ,chemistry ,Indicators and Reagents ,MESH: Female - Abstract
Amidoxime and O-substituted derivatives of the bis-alkylamidine 1,12-bis(N,N'-acetamidinyl)dodecane were synthesized and evaluated as in vitro and in vivo antimalarial prodrugs. The bis-O-methylsulfonylamidoxime 8 and the bis-oxadiazolone 9 derivatives show relatively potent antimalarial activity after oral administration.
- Published
- 2007
32. 1-(2-Methylimidazo[1,2-a]pyridin-3-yl)-3,3-bis(methylsulfanyl)prop-2-enone monohydrate
- Author
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R. C. A. Yao-Kakou, Yvon Bibila Mayaya Bisseyou, Mahama Ouattara, Severin D. Goulizan Bi, and Drissa Sissouma
- Subjects
Crystallography ,Hydrogen bond ,Chemistry ,General Chemistry ,Condensed Matter Physics ,Bioinformatics ,Medicinal chemistry ,Organic Papers ,Absolute deviation ,Crystal ,chemistry.chemical_compound ,QD901-999 ,Pyridine ,General Materials Science ,Enone - Abstract
The title compound, C13H14N2OS2·H2O, appears in the form of bimolecular aggregate in which molecular components are linked by O—H...N hydrogen bonding. The nine-membered imidazo[1,2-a]pyridine system is almost planar, with a mean deviation of 0.026 (1) Å. An intramolecular C—H...O hydrogen bond forms within the imidazo[1,2-a]pyridine system. The crystal packing is consolidated by O—H...O and C—H...O hydrogen bonds, forming a supramolecular structure consisting of perpendicular infinite molecular chains running along the a and c axes.
- Published
- 2009
33. Potent Antimalarial Activity of 2-Aminopyridinium Salts, Amidines, and Guanidines.
- Author
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Michèle Calas, Henri Vial, Mahama Ouattara, Gilles Piquet, Zyta Ziora, Y. Bordat, Marie L. Ancelin, and Roger Escale
- Published
- 2007
- Full Text
- View/download PDF
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