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Identifying novel lead compounds in drug discovery has been challenging because of the rapid rise of drug resistance to the existing chemotherapeutics and a lack of understanding of complex metabolic pathways in the parasite. Integrating computational and experimental approaches has shown to be of great worth in identifying and developing novel promising pharmacophore hybrids. In this present research, a series of new 4-(1H)-pyridone-derived antimalarial agents were designed based on recent reports and our preliminary findings through in-silico studies. Two of the 4-(1H)-Pyridone derivatives showed potential to bind to the Q0 site of the cytochrome bc1 complex and disrupt the mitochondrial electron transport chain. These compounds, along with previously synthesized compounds, exhibited significant inhibitory activities against the malaria parasite. Presently, seven compounds were successfully synthesized, characterized and these novel compounds have shown promise as antimalarial agents.

Quinoline, which consists of benzene fused with N-heterocyclic pyridine, has received considerable attention as a core template in drug design because of its broad spectrum of bioactivity.

The “National Home Growing School Feeding Program” by Nigeria government was designed to overcome malnutrition disorders through regular school-feeding to improve the nutrition status and the education abilities of school children. Hence, this study focused on assessing the effect of ‘national home growing school feeding program’ on the nutritional status of children of rural households in Osun State, Nigeria. Primary data was used for the study. Two stage random sampling was used for the study, the first stage which was the random selection of four (4) rural communities from each of the three (3) Agro-ecological zones present in the state and the second stage was the random sampling of 10 households from each of the selected communities, comprising of households whose children are beneficiaries and not beneficiaries of the program. A total of 120 households were used for the study. A structured questionnaire was used for the purpose of extracting needed information from the respondents. The data collected was analyzed using Descriptive Statistics, Anthropometry, Logistics Regression Model and Chi-square Analysis. Result of analysis revealed that nutritional status of children in the study area is significantly influenced by child’s sex, child’s age, mother’s education, national home growing school feeding program, access to clean water, access to sanitation facilities and household income. The effect of national home growing school feeding program on the nutritional status of the children was statistically significant (chi-square=37.263, p < 0.000) which means the program has positive effect on the nutritional status of children in the study area. The study therefore recommended that government should ensure the sustenance of National Home Growing School Feeding Program especially in the rural areas of the country. Education of the rural women folks should be taken importantly by governments and NGOs as they are the one directly taking care of children wellbeing. Government, NGOs and Community groups should Journal of the Faculty of Agriculture and Veterinary Medicine, Imo State University Owerri also provide the basic amenities like portable water supply and sanitation facilities in the rural areas so as to curb the incidence of diseases and malnutrition. Keywords: National Home Grown School Feeding Program, Nutritional Status, Health, Malnutrition

Microwave-assisted approach was utilized as green approach to access a series of 2-propylquinoline-4-carbohydrazide hydrazone derivatives 10a-j of aromatic and heteroaromatic aldehydes in highly encouraging yields. It involved four steps reaction which was initiated with ring opening reaction of isatin in a basified environment and subsequent cross-coupling with pentan-2-one to produce compound 7. Esterification of 7 in acid medium led to the formation of compound 8 which was reacted with hydrazine hydrate to access 9 which upon microwave-assisted condensed with aromatic and heteroaromatic aldehydes furnished the targeted compounds 10a-j. The structures of 10a-j were confirmed by physico-chemical, elemental analyses and spectroscopic characterization which include UV, FT-IR, 1H and 13C NMR as well as DEPT-135. The targeted compounds 10a-j, alongside with gentamicin clinical standard, were investigated for their antibacterial efficacies using agar diffusion method. 2-Propyl-N′-(pyridine-3-ylmethylene) quinoline-4-carbohydrazide 10j emerged as the best antibacterial hydrazide-hydrazone with lowest MIC value of 0.39 ± 0.02 – 1.56 ± 0.02 µg/mL across all the organisms screened. Keywords: Pfitzinger synthesis, Microwave irradiation, Quinoline, Spectral study, Antibacterial

This study describes the qualitative phytochemical screening, antimicrobial and GC-MS analyses of the crude methanol extract of the stem and roots parts of Bidens pilosa partitioned between methanol, dichloromethane, ethyl acetate and hexane solvents. Phytochemical analysis indicated the presence of cardiac glycosides, terpenoids, flavonoids and alkaloids. Saponins were not found in any of the fractions of stem and root of B. pilosa. Antibacterial studies indicated that the lowest concentration (6.25 mg/mL) was achieved for Candida subtilis for the ethyl acetate fraction of the stem extract and hexane fraction of the root extract. Antimycobacterial test activity of these solvent fractions revealed that the hexane fraction of the root extract was susceptible to the bacterium isolate. Gas chromatography-Mass spectrometric study revealed the presence of the following compounds - cis-9-Hexadecenal, 2-hydroxyl ethyl (Z)-9-Octadecenoate, Octadecanal, Oleic acid, 4-(dimethylamino)-Benzaldehyde, 4,6,7-Trimethoxy-2,3-dihydrofuro(2,3-b)quinolone.

Surpassing heart diseases, cancer is taking the lead as the deadliest disease because of its fast rate of spreading in all parts of the world. Tireless commitment to searching for novel therapeutic medicines is a worthwhile adventure in synthetic chemistry because of the drug resistance predicament and regular outbreak of new diseases due to abnormal cell growth and proliferation. Medicinal chemistry researchers and pharmacists have unveiled quinoxaline templates as precursors of importance and valuable intermediates in drug discovery because they have been established to possess diverse pharmacological potentials. Hence, this review highlights the current versatile routes to accessing functionalized quinoxaline motifs and harnessing their documented therapeutic potentials for anticancer drug development.

A variety of 3-(5-(substituted-phenyl)-4,5-dihydro-1H-pyrazol-3-yl)-2H-chromen-2-one derivatives 3a–j were synthesized through microwave assisted thermal annulation of corresponding α,β-unsaturated ketones (chalcones) 2a–j via hydrazinolysis. Chalcones 2a–j were prepared from 3-acetyl-coumarin 1 which was previously accessed by Pechmann condensation reaction of salicylaldehyde. The series of pyrazoline-based coumarin motifs 3a–j synthesized, were structurally confirmed by analytical and spectral data. They were then evaluated for their antimicrobial activities using agar diffusion method. The result showed that microwave assisted method (MAM) for the reaction was remarkably successful and gave the targeted products 3a–j in higher yields at shorter reaction times compared to conventional synthetic method (CSM). The results showed that these skeletal frameworks exhibited marked potency as antibacterial agents. The most active antibacterial agent was 3-(5-(4-(diethylamino) phenyl)-4,5-dihydro-1H-pyrazol-3-yl)-2H-chromen-2-one 3j with MIC and MBC values of 3.92 ± 0.22 µg/mL and 7.82 ± 0.43 µg/mL respectively.

Plants are the world's most consumed goods. They are of high economic value and bring many health benefits. In most countries in Africa, the supply and quality of food will rise to meet the growing population's increasing demand. Genomics and other biotechnology tools offer the opportunity to improve subsistence crops and medicinal herbs in the continent. Significant advances have been made in plant genomics, which have enhanced our knowledge of the molecular processes underlying both plant quality and yield. The sequencing of complex genomes of African plant species, facilitated by the continuously evolving next-generation sequencing technologies and advanced bioinformatics approaches, has provided new opportunities for crop improvement. This review summarizes the achievements of genome sequencing projects of endemic African plants in the last two decades. We also present perspectives and challenges for future plant genomic studies that will accelerate important plant breeding programs for African communities. These challenges include a lack of basic facilities, a lack of sequencing and bioinformatics facilities, and a lack of skills to design genomics studies. However, it is imperative to state that African countries have become key players in the plant genome revolution and genome derived-biotechnology. Therefore, African governments should invest in public plant genomics research and applications, establish bioinformatics platforms and training programs, and stimulate university and industry partnerships to fully deploy plant genomics, particularly in the fields of agriculture and medicine.

Microwave-assisted organic synthesis has emerged as a sustainable technique for the preparation of valuable material for societal needs. Microwave-assisted approach is environmentally friendly and green method of synthesis because of the simple experimental procedure, short reaction time, accelerated reaction rate, prevention of hazardous chemical discharge, and improved product yields, which are the added advantages over conventional heating method under reflux. This present work unveils the microwave-assisted as an essential toolbox and viable energy source for accessing various condensation reactions which are of paramount importance to a man in the industrial process, drug discovery, and material science research for technological advancement. Thus, critical and deep insight into microwave-assisted condensation reactions are herein highlighted in order to stimulate the interest of more synthetic chemists in the prolific engagement of microwave-assisted approach in the development of more efficient and sustainable chemical transformations.

We report the plant-mediated synthesis, structural investigation, optical properties and theoretical modelling of a triclinic (anorthic) phase AgCoPO4 nanoparticles for the first time. As part of green chemistry, the secondary metabolites in the leaf extract of Canna indica were engaged as the reducing/capping agent for the metal nanoparticles. X-ray diffraction (XRD) revealed the presence of an anorthic AgCoPO4 phase, crystallised in a triclinic structure with P -1 space group. Optical studies using UV-vis spectroscopy and photoluminescence are reported. Transmission electron microscopy suggests the formation of quasi-nanocube morphology, unlike the conventional spherically-shaped nanoparticles via plant-mediated reduction method. Elemental composition of the nanohybrid was confirmed by energy-dispersive x-ray spectroscopy (E.D.S.). Evidence of crystallinity was supported by selected area electron diffraction (SAED). Study of the dynamic anisotropy of the nanohybrid at optimised state suggests its proposed application as optical material in colourimetric metal nanoparticles-mediated sensors.

Schiff bases have continued to gain attention as essential building blocks and versatile pharmacophores in drug development and drug-like molecular entities. Thus, the synthesis of Schiff bases was achieved herein via facile acetic acid catalyzed synthetic transformation of chalcones. The targeted Schiff bases and related compounds 2a-m were accessed by the treatment of amines with chalcone 1 which was previously derived through Claisen-Schmidt reaction between benzaldehyde and acetone, at ambient temperature. Structural characterization was achieved via physicochemical properties and the use of IR, UV, 1H and 13C NMR which were spectroscopic techniques. The compounds have essential candidature for further study, in biological activity so as to unleash their medicinal potential.

Malaria remains one of the most infectious life-threatening diseases in the world. The lingering effect of drug resistance by malarial parasites, especially Plasmodium falciparum, has made it essential for the continuous search for novel antimalarial drugs that can act on new protein targets and through new modes of action. Amidoxime functional groups have, in recent years, shown to be good incorporations in heterocyclic backbones due to their vast biological activities. Hence, the antimalarial activities of some amidoxime-containing heterocyclic compounds have been predicted using molecular docking studies to determine the binding affinities and the inhibition constants of the compounds. The amidoxime-containing compounds were downloaded from the ZINC database and docked, using Auto Dock vina, against the active sites of homology modelled Plasmodium falciparumadenylosuccinate lyase (PfADSL) as obtained from the SWISS-MoDeL. The grid box was constructed using 80, 80, and 80, pointing in x, y, and z directions, respectively, with a grid point spacing of 0.375 A. The post-docking analysis, which entails determining the hydrogen bond formed and the bond length between the compounds and the protein target, was carried out using AutoDockTools, LigPlot and PyMOLmolecular viewer. The docking studies showed that the compounds possess binding affinities ranging from -8.6 to- 5.7 kcal/mol, with ZINC2268942 having the lowest binding affinity. The presence of the amidoxime-functional group on the best hit contributed significantly to the hydrogen bonds formed between the compound and the binding sites of PfADSL,which were observed atThr 124D, Ser 125D, Thr 172C, His 173C, Gln 250D, and Ser 299A. The results obtained from the molecular docking studies will be helpful in the development of a potential antimalarial drug that can target PfADSL after careful experimental validation of the target, then in vitro and in vivo screening.

The pursuit for bioremediation has led to alternative route for the synthesis of nanoparticles and their hybrids. Data in this article display optical properties and progress in the formation of silver and silver/nickel bimetallic nanoparticles using eco-friendly reducing agent (Akinsiku et al. 2018). The as-prepared nanoparticles portrayed nanocrystalline nature as revealed in the x-ray powder diffraction (XRPD) data. Data also exposed antimicrobial activity of the synthesized nanoparticles.

In the quest for environmental remediation which involves eco-friendly synthetic routes, we herein report synthesis and modeling of silver nanoparticles (Ag NPs) and silver/nickel allied bimetallic nanoparticles (Ag/Ni NPs) using plant-extract reduction method. Secondary metabolites in the leaf extract of Canna indica acted as reducing agent. Electronic transitions resulted in emergence of surface plasmon resonance in the regions of 416 nm (Ag NPs) and 421 nm (Ag/Ni NPs) during optical measurements. Further characterizations were done using TEM and EDX. Antimicrobial activity of the nanoparticles against clinical isolates was highly significant as P<0.05. These findings suggest application of Ag NPs as antibacterial agent against E. coli, S. pyogenes, and antifungal agent against C. albicans. Possible antibacterial drugs against S. pyogenes and E. coli can also be designed using Ag/Ni nanohybrid based on their strong inhibition activities. Similarly, the enhanced SPR in the nanoparticles is suggested for applications in optical materials, as good absorbers and scatters of visible light. Theoretical model clarified that the experiment observation on the relationship between metallic nanoparticles penetration through peptidoglycan layers and the activeness of microbial species depends on the nature of the nanoparticles and pore size of the layer.

The World Academy of Sciences (TWAS) was gratefully acknowledged by OOA for the sponsorship of this present work under the TWAS Research Grant for Individual Scientists in Basic Sciences Programme (grant no.: 14-069 RG/CHE/AF/AC_1).

The aim of this present study was to synthesize 2-substituted and 1,2-disubstituted benzimidazole derivatives to investigate their antibacterial diversity for possible future drug design. The structure-based design of precursors 2-(1H-benzimidazol-2-yl)aniline 1, 2-(3,5-dinitro phenyl)-1H-benzimidazole 3 and 2-benzyl-1H-benzimidazole 5 were achieved by the condensation reaction of o-phenylenediamine with anthranilic acid, 3,5-dinitrophenylbenzoic acid, and phenylacetic acid, respectively. The precursors 1, 3 and 5, upon reaction with six different electrophile-releasing agents, furnished the corresponding 2-substituted benzimidazole, 2a-f and 1,2-disubstituted benzimidazole derivatives 4a-f and 6a-f, respectively. The structural identity of the targeted compounds was authenticated by elemental analytical data and spectral information from FT-IR, UV, 1H, and 13C NMR. The outcome of the findings from the in vitro screening unveiled 2-benzyl-1-(phenylsulfonyl)-1H-benzimidazole 6b as the most active derivative with lowest MIC value of 15.63 µg/mL.

Quinazoline and quinazolinone derivatives are well-known bioactive heterocycles owing to their therapeutic diversity and extensive medicinal application in drug design and pharmaceutics. A series of 2-methyl-3-substituted quinazolin-4(3H)-one derivatives 8a-q was herein synthesized from synthetic conversion of anthranilic acid to 2-methyl-4H-3,1-benzoxazi-4-one, 7 which was subsequently transformed to the targeted 2,3-disubstituted quinazolin-4(3H)-one derivatives 8a-q by reacting with some notable amino-containing moieties via an ameliorable pathway. The catalyst-free synthesis was successful achieved by careful reaction optimization study using solvent choice and reaction temperature variability as key parameters. The chemical structures of the synthesized compounds were confirmed by IR, UV, 1H-NMR, 13C-NMR and DEPT-135 as well as analytical data.

This review examines the unparalleled chemical and physical properties of ZnO nanoparticles and its hybrid forms. The influence of these multifunctional materials within the polymeric matrix of organic coatings was discussed. The scanning electron microscope is seen to provide relevant information about the dispersion of the hybrid and composite coating systems. This review provides concise information about the antimicrobial and thermal stability of composites.

Plasmodium falciparum adenylosuccinate lyase ( Pf ADSL) is an important enzyme in purine metabolism. Although several benzimidazole derivatives have been commercially developed into drugs, the template design as inhibitor against Pf ADSL has not been fully explored. This study aims to model the 3-dimensional (3D) structure of Pf ADSL, design and predict in silico absorption, distribution, metabolism, excretion and toxicity (ADMET) of 8 substituted benzo[ d ]imidazol-1-yl)methyl)benzimidamide compounds as well as predict the potential interaction modes and binding affinities of the designed ligands with the modelled Pf ADSL. Pf ADSL 3D structure was modelled using SWISS-MODEL, whereas the compounds were designed using ChemDraw Professional. ADMET predictions were done using OSIRIS Property Explorer and Swiss ADME, whereas molecular docking was done with AutoDock Tools. All designed compounds exhibited good in silico ADMET properties, hence can be considered safe for drug development. Binding energies ranged from −6.85 to −8.75 kcal/mol. Thus, they could be further synthesised and developed into active commercial antimalarial drugs.

Plasmodium falciparum adenylosuccinate lyase ( PfADSL) is an important enzyme in purine metabolism. Although several benzimidazole derivatives have been commercially developed into drugs, the template design as inhibitor against PfADSL has not been fully explored. This study aims to model the 3-dimensional (3D) structure of PfADSL, design and predict in silico absorption, distribution, metabolism, excretion and toxicity (ADMET) of 8 substituted benzo[ d]imidazol-1-yl)methyl)benzimidamide compounds as well as predict the potential interaction modes and binding affinities of the designed ligands with the modelled PfADSL. PfADSL 3D structure was modelled using SWISS-MODEL, whereas the compounds were designed using ChemDraw Professional. ADMET predictions were done using OSIRIS Property Explorer and Swiss ADME, whereas molecular docking was done with AutoDock Tools. All designed compounds exhibited good in silico ADMET properties, hence can be considered safe for drug development. Binding energies ranged from −6.85 to −8.75 kcal/mol. Thus, they could be further synthesised and developed into active commercial antimalarial drugs.

Geophysical investigation and microstudy of soil properties were carried out within Bowen University, for the characterization of the subsurface pattern in the area using vertical electrical sounding (VES) survey and evaluation of soil properties with a view to mapping subsurface geological features, such as weak and competent zones and to determine the overburden thickness of the area for pre-foundation studies for a proposed high-rise building. Four (4) VES was carried out in the study area employing schlumberger electrode configuration. The data collected were used to curve match and the results used for subsequent interpretation to reveal the depth, thickness and resistivity of the study area. In addition, soil samples were collected from three (3) selected points located at the entrance, centre and the end of the study area at about a depth 0-60 cm. Consequently, the VES results were presented as resist graph, which revealed the range of values for the depth (1.3 – 24.5), thickness (1.3 – 15.4 m) and resistivity (357.4 - 6311.6 ohms), which was later used to generated the geoelectric maps of the study area. It was also observed that the result of the soil properties revealed that all the samples taken from the study area have low bulk density (1.41 g/cm 3 , 1.26 g/cm 3 , 1.36 g/cm 3 ), high particle density (2.81 g/cm 3 , 2.94 g/cm 3 , 3.16 g/cm 3 ), and high porosity (49.64%, 57.22%, 57.03%). In conclusion, it was observed that erection of high-rise building is not advisable within the study area since the results showed that the overburden (depth to basement) is generally thick mostly greater than 15 m. Also revealed from the microstudy of soil properties is that foundation stability should be properly managed, since a porous soil does not accommodate engineering activities except when an artificial basement is put in place. Keywords : Geophysical Investigation, Soil Analysis, Foundation Studies, Subsurface Competency

There are many varieties of seeds and nuts that can produce oils for food, nutraceuticals, skin care prod-ucts, aromatherapies, fuels and industrial lubricants. In this present study, the oil from the seed of Caryota mitis was extracted by soxhlet extraction and investigated to promote its quality aspects for biodiversity. The structural characterization of the oil was carried out using physico-chemical analyses and spectroscopic means such as FR-IR, 1H and 13C-NMR as well as mass spectral data. The phytochemical screening of the oil from Caryota mitis seed species revealed the presence of phytosterols, triterpenes, alkaloids, flavonoids and saponins. The proximate analysis showed the moisture content to be 42%, while crude fibre, carbohydrate, crude fat, crude protein and ash content was found to be 34.30%, 11.92%, 5.30%, 4.64% and 1.84% respectively on dry matter basis. The mineral content determination revealed the presence of iron (3.10 ± 0.02 mg/kg), manganese (0.11 ± 0.01 mg/kg), sodium (154.15 ± 1.98 mg/kg) and potassium (127.04 ± 1.21 mg/kg) while cadmium, nickel and lead were not detected. The in vitro antimicrobial screening on the oil, showed that it has promising antimicrobial potential on the organism tested but it was not as active as the clinical standards used. This oil is therefore, a candidate for further study in terms of the cytotoxicity profile and its ability to be used as functional food for proper exploration of its nutraceutical endowment.

Benzimidazole derivatives are crucial structural scaffolds found in diverse libraries of biologically active compounds which are therapeutically useful agents in drug discovery and medicinal research. They are structural isosteres of naturally occurring nucleotides, which allows them to interact with the biopolymers of living systems. Hence, there is a need to couple the latest information with the earlier documentations to understand the current status of the benzimidazole nucleus in medicinal chemistry research. This present work unveils the benzimidazole core as a multifunctional nucleus that serves as a resourceful tool of information for synthetic modifications of old existing candidates in order to tackle drug resistance bottlenecks in therapeutic medicine. This manuscript deals with the recent advances in the synthesis of benzimidazole derivatives, the widespread biological activities as well as pharmacokinetic reports. These present them as a toolbox for fighting infectious diseases and also make them excellent candidates for future drug design.

Background: This study was carried out to investigate proximate composition, phytochemical profile and antimicrobial activity of the spectroscopically characterized seed oil of Bauhinia tomentosa . Materials and method: The characterization was carried out using FT-IR, mass spectra, 1H- and 13C-NMR. Results: The results from the proximate analysis showed the presence of crude protein 30.36±0.98%, crude fibre 26.00±0.69%, carbohydrate 25.32±0.57%, moisture content 12.04±0.39%, ash content 4.00±0.15% and fat content 2.28±0.09%. The phytochemical screening revealed the presence of alkaloids, flavonoids, saponins, terpenes, cardiac glycosides, sterols, anthraquinones and tannins in varying degrees. The mineral determination showed that the seed oil contained iron (3.10±0.01 mg kgG1), manganese (0.38±0.01 mg kgG1), while cadmium (0.0 mg kgG1), lead (0.0 mg kgG1) and nickel (0.0 mg kgG1) were not detected. The extracted seed oil was investigated for antimicrobial efficiency against four bacterial isolates and two fungal, wherein gentamicin and clotrimazole were the clinical standard antibiotic and antifungal agents, respectively. Conclusion: The antimicrobial activity result revealed the sample to be bioactive and of great pharmaceutical potential with MIC value of 6.25 and

In this study, 3-acetylcoumarin 1, used as the essential precursor was synthesized by the reaction of salicyaldehyde with ethyl acetoacetate in the presence of a catalytic amount of piperidine in solvent-free medium. Schiff bases 2-9 were obtained by the condensation reaction of 3-acetylcoumarin, 1 with various aniline derivatives while reaction of 3-hydrazinoquinoxalin-2-one with four different 6-susbtituted 3-acetylcoumarins afforded the corresponding hydrazones 10-13. Both Schiff bases and hydrazone products were synthesized under microwave irradiation method and conventional synthetic strategy for comparative study. The microwave assisted reaction was remarkably successful and gave both Schiff bases and hydrazones in higher yields at shorter reaction time compared to conventional heating method. The characterization of the synthesized compounds were structurally confirmed by analytical data as well as spectroscopic means which involved 1H-and 13C-nmr, ir, UV-visible and mass spectra.

1,3,4-oxadiazole derivatives have shown to have diverse and vast applications, from medicinal chemistry for the treatment and possible treatment of various ailments to its application in the industrial development when used as corrosion inhibitions and light emitting diodes. These diverse applications can be as a result of the numerous viable synthetic pathways illustrated in this review. 1,3,4-oxadiazoles can be synthesized in very high yields, using green approaches and having various life-changing applications. This review explores the various recent synthetic routes available for the development of 1,3,4-oxadiazoles and their biological activities.

Resistance of the malaria parasite to conventional therapeutic agents calls for increased efforts in antimalarial drug discovery. Current efforts should be targeted at developing safe and affordable new agents to counter the spread of malaria parasites that are resistant to existing therapy. In this study, toxicological and in vivo antiplasmodial properties of 3-(5-(s-phenyl)-4H-pyrazol-3-yl)-42H-chromen-2, Mangifera indica and Tithonia diversifolia in swiss albino mice models, Musmusculus were investigated. 2H-Chromen-2-one also known as coumarin is highly privileged oxygencontaining heterocyclic entity which are present in plant kingdom as secondary metabolites. The maceration technique of crude drug extraction was employed using cold water extraction. Toxicological analysis was carried out using Lorke’s method for acute toxicity testing while the chemosuppressive activity was carried out using Peter’s four day test on early infection. We also report the synthesis of functionalized 3-(5-(s-phenyl)-4H-pyrazol-3-yl)-2H-chromen-2-one motifs via microwave assisted synthetic approach and isolation of indigenous plant extract in order to investigate their antimalarial efficacy. The condensation reaction of 3-acetylcoumarin with various benzaldehyde derivatives resulted in the formation of 3-[3-acryloyl]-2H-chromen-2-one which was subsequently reaction the hydrazine hydrate via microwave assisted hydrazinolysis to afford the targeted 3-(5-(s-phenyl)-4H-pyrazol-3-yl)-2H-chromen-2-one motifs. The chemical structures were confirmed by analytical data and spectroscopic means such as FT-IR, UV, 1H NMR, 13C NMR and DEPT-135. The microwave assisted reaction was remarkably successful and gave targeted 3-(5-(s-phenyl)-4H-pyrazol-3-yl)-2H-chromen- 2-one motifs in higher yields at lesser reaction time compared to conventional heating method. The LD50 of the aqueous extracts of the leaves and stem bark Mangifera indica was established to be ± 707.11 mg/kg b.w., p.o. (body weight, administered orally) in mice. Tithonia diversifolia aqueous leaf extracts is non-toxic at doses as high as 1000 mg/kg while the LD50 of the ethanolic leaf extracts was established to be ± 707.11 mg/kg b.w., p.o. in mice. The in vivo antiplasmodial activity was studied in chloroquine-sensitive Plasmodium berghei berghei - NK65 infected mice. All the plant extracts, at the doses (100, 200 and 400 mg/kg b.w., p.o.) used, produced significant (p 80% inhibition of parasitaemia at maximum dose) against the parasite in the suppressive tests. The in vitro antimalarial screening of the synthesized compounds is presently on-going and the finding will be reported in due course.

Background and Objective: Sulfonamides are known to represent a class of medicinally important compounds and chemical intermediates, which are extensively used in drug development. The aim of this present study is to synthesize a series of arylsulfonamide-based dialkylated amide motifs. Materials and Methods: In this study, the design and development of arylsulfonamide pharmacophore bearing N,N-diethyl substituted amide moieties 2a-k was achieved in improved yields using non-conventional amidation of p-tolylsulfonamide precursors 1a-k. The structures of the compounds were substantiated based on the results of elemental analysis and spectroscopic data namely, FT-IR, 1H-NMR, 13C-NMR and mass spectra. Results: The series of targeted compounds were synthesized in good to excellent yields and subsequently purified by column chromatography where necessary. Conclusion: The synthesis of arylsulfonamide-based dialkylated amide motifs was successfully achieved. These compounds may serve as versatile intermediates that pave ways toward achieving diverse bioactive heterocyclic compounds for future drug discovery and development.

The pyrimidine moiety is one of the most widespread heterocycles in biologically occurring compounds, such as nucleic acids components (uracil, thymine and cytosine) and vitamin B1. Due to its prebiotic nature to living cells in biodiversity, it is an highly privileged motif for the development of molecules of biological and pharmaceutical interest. This present work deals with the exploration of chemistry and medicinal diversity of pyrimidine which might pave way to long await discovery in therapeutic medicine for future drug design.

A series of functionalized 2-substituted benzimidazole motifs was designed and successfully synthesized via thermal cyclization of 1,2-diaminobenzene on COOH end of L- leucine to achieve benzimidazole derivatives 6 as the essential precursor. The coupling of the precursor 6 with benzaldehyde derivatives a-h, ketone series i-k, and aryl sulfonyl chlorides l-n led to the formation of the targeted 2-substituted benzimidazole motifs 7a-n in improved yields. The targeted benzimidazole motifs were structurally authenticated through their spectral data and microanalytical parameters. The targeted final moieties were investigated for potential antimicrobial activity using the agar diffusion method with gentamicin as the clinical standard. All the compounds had a broad spectrum of activity with compound 7k having the highest remarkable activity with MIC of 0.98 ± 0.02 µg/mL and MBC value of 3.91 ± 0.10 µg/mL. These findings suggest that compound 7k containing camphor might be a good candidate for the design of new antimicrobial small-molecule drugs.

Medicinal plant research is a highly diversified topic of interest owing to applications of their phytoconstituents in drug discovery, human dietary intake, corrosion inhibition, material science research among others. The study revealed the phytochemical composition and proximate determination of Pentaclethra macrophylla benth (African oil bean) seed. The dried seeds of Pentaclethra macrophylla benth were pulverized into fine powder and a portion of it was extracted with n-hexane. The result of the phytochemical screening of the extract from Pentaclethra macrophylla showed that the oil seeds contained terpenoids, cardiac glycosides and saponin while steroids, alkaloids, flavonoids, tannins, phlabotannins and anthraquinones were not detected. Proximate analysis indicated low moisture content (1.895 %), while other parameter determined include ash (2.033%), crude fibre (17.227%), acid value (8.182), iodine value (101.235), peroxide value (20.06), and free fatty acid (4.091). This extract is a candidate with potential for further study regarding unveiling of their mechanical properties for technological advances.