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6 results on '"Gilbert Umuhire, Mahoro"'

1. Neuropathic pain-alleviating activity of novel 5-HT

Author

Marcin, Drop, Florian, Jacquot, Vittorio, Canale, Severine, Chaumont-Dubel, Maria, Walczak, Grzegorz, Satała, Klaudia, Nosalska, Gilbert Umuhire, Mahoro, Karolina, Słoczyńska, Kamil, Piska, Sylvain, Lamoine, Elżbieta, Pękala, Nicolas, Masurier, Andrzej J, Bojarski, Maciej, Pawłowski, Jean, Martinez, Gilles, Subra, Xavier, Bantreil, Frédéric, Lamaty, Alain, Eschalier, Philippe, Marin, Christine, Courteix, and Paweł, Zajdel

Subjects
Male, Structure-Activity Relationship, Dose-Response Relationship, Drug, Molecular Structure, Receptors, Serotonin, Animals, Humans, Neuralgia, Pyrroles, Serotonin Antagonists, Rats, Wistar, Cell Line, Rats
Abstract

The diverse signaling pathways engaged by serotonin type 6 receptor (5-HT

Published
2021

2. Neuropathic pain-alleviating activity of novel 5-HT6 receptor inverse agonists derived from 2-aryl-1H-pyrrole-3-carboxamide

Author

Gilles Subra, Maciej Pawłowski, Paweł Zajdel, Marcin Drop, Kamil Piska, Philippe Marin, Jean Martinez, Florian Jacquot, Alain Eschalier, Andrzej J. Bojarski, Karolina Słoczyńska, Vittorio Canale, Christine Courteix, Gilbert Umuhire Mahoro, Grzegorz Satała, Klaudia Nosalska, Xavier Bantreil, Nicolas Masurier, Elżbieta Pękala, Sylvain Lamoine, Séverine Chaumont-Dubel, Maria Walczak, Frédéric Lamaty, 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), Uniwersytet Jagielloński w Krakowie = Jagiellonian University (UJ), Neuro-Dol (Neuro-Dol), Institut National de la Santé et de la Recherche Médicale (INSERM)-Université Clermont Auvergne (UCA), Institut de Génomique Fonctionnelle (IGF), Institut National de la Santé et de la Recherche Médicale (INSERM)-Université de Montpellier (UM)-Centre National de la Recherche Scientifique (CNRS), Jagiellonian University - Medical College, ANR-17-CE16-0010,Sero6Dev,Réseau de signalisation associé au récepteur 5-HT6 et développement neuronal(2017), ANR-17-CE16-0013,StopSero6TOR,La signalisation mTOR induite par le récepteur 5-HT6 comme cible thérapeutique pour prévenir l'apparition des déficits cognitifs dans la schizophrénie(2017), ANR-19-CE18-0018,SERO6Pain,Les voies de signalisation du récepteur 5-HT6: de nouvelles cibles pour le traitement de la douleur neuropathique?(2019), ANR-18-CE18-0018,SMARt-TB,Molécules de réversion de la résistance aux prodrogues chez M. tberculosis(2018), and Université de Montpellier (UM)-Université Montpellier 1 (UM1)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Université Montpellier 2 - Sciences et Techniques (UM2)-Centre National de la Recherche Scientifique (CNRS)

Subjects
Cdk5 signaling, [SDV.NEU.NB]Life Sciences [q-bio]/Neurons and Cognition [q-bio.NC]/Neurobiology, Analgesic, [CHIM.THER]Chemical Sciences/Medicinal Chemistry, Pharmacology, Neuropathic pain, Biochemistry, 5-HT(6) receptor inverse agonism, 03 medical and health sciences, 0302 clinical medicine, Drug Discovery, Inverse agonist, Receptor, Flow chemistry, Molecular Biology, PI3K/AKT/mTOR pathway, 030304 developmental biology, ADME, 0303 health sciences, Chemistry, Organic Chemistry, 3. Good health, Spinal nerve ligation, mTOR kinase, [SDV.SP.PHARMA]Life Sciences [q-bio]/Pharmaceutical sciences/Pharmacology, 5-HT6 receptor, Signal transduction, 030217 neurology & neurosurgery
Abstract

International audience; The diverse signaling pathways engaged by serotonin type 6 receptor (5-HT6R) together with its high constitutive activity suggests different types of pharmacological interventions for the treatment of CNS disorders. Nonphysiological activation of mTOR kinase by constitutively active 5-HT6R under neuropathic pain conditions focused our attention on the possible repurposing of 5-HT6R inverse agonists as a strategy to treat painful symptoms associated with neuropathies of different etiologies. Herein, we report the identification of compound 33 derived from the library of 2-aryl-1H-pyrrole-3-carboxamides as a potential analgesic agent. Compound 33 behaves as a potent 5-HT6R inverse agonist at Gs, Cdk5, and mTOR signaling. Preliminary ADME/Tox studies revealed preferential distribution of 33 to the CNS and placed it in the low-risk safety space. Finally, compound 33 dose-dependently reduced tactile allodynia in spinal nerve ligation (SNL)-induced neuropathic rats.

Published
2021
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3. Novel Red‐Emitting Copper(I) Complexes with Pyrazine and Pyrimidinyl Ancillary Ligands for White Light‐Emitting Electrochemical Cells

Author

Jean-François Lohier, Luca M. Cavinato, Gilbert Umuhire Mahoro, Sylvain Gaillard, Jean-Luc Renaud, Elisa Fresta, and Rubén D. Costa

Subjects
chemistry.chemical_compound, Materials science, chemistry, Pyrazine, White light, chemistry.chemical_element, Photochemistry, Copper, Atomic and Molecular Physics, and Optics, Electronic, Optical and Magnetic Materials, Electrochemical cell
Published
2021
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4. Recent advances in solid‐state lighting devices using transition metal complexes exhibiting thermally activated delayed fluorescent emission mechanism

Author

Pedro B. Coto, Julio Fernandez-Cestau, Sylvain Gaillard, Gilbert Umuhire Mahoro, Rubén D. Costa, Jean-Luc Renaud, Centre National de la Recherche Scientifique (France), Agence Nationale de la Recherche (France), Comunidad de Madrid, European Research Council, European Commission, Fundación BBVA, Laboratoire de chimie moléculaire et thioorganique (LCMT), Centre National de la Recherche Scientifique (CNRS)-Institut Normand de Chimie Moléculaire Médicinale et Macromoléculaire (INC3M), Institut de Chimie du CNRS (INC)-École Nationale Supérieure d'Ingénieurs de Caen (ENSICAEN), Normandie Université (NU)-Normandie Université (NU)-Institut national des sciences appliquées Rouen Normandie (INSA Rouen Normandie), Institut National des Sciences Appliquées (INSA)-Normandie Université (NU)-Institut National des Sciences Appliquées (INSA)-Université Le Havre Normandie (ULH), Normandie Université (NU)-Université de Rouen Normandie (UNIROUEN), Normandie Université (NU)-Centre National de la Recherche Scientifique (CNRS)-Université de Caen Normandie (UNICAEN), Normandie Université (NU)-Institut de Chimie du CNRS (INC)-École Nationale Supérieure d'Ingénieurs de Caen (ENSICAEN), Normandie Université (NU), Institute IMDEA Materials [Madrid], Institute IMDEA Materials, and University of Oviedo

Subjects
Materials science, [CHIM.ORGA]Chemical Sciences/Organic chemistry, Nanotechnology, [CHIM.CATA]Chemical Sciences/Catalysis, [CHIM.MATE]Chemical Sciences/Material chemistry, 02 engineering and technology, 010402 general chemistry, 021001 nanoscience & nanotechnology, 01 natural sciences, Fluorescence, Atomic and Molecular Physics, and Optics, 0104 chemical sciences, Electronic, Optical and Magnetic Materials, law.invention, Solid-state lighting, Transition metal, law, Theoretical methods, OLED, 0210 nano-technology
Abstract

This review focuses on the state‐of‐the‐art of solid‐state lighting devices (SSLDs)—that is, organic light‐emitting diodes (OLEDs) and light‐emitting electrochemical cells (LECs)—prepared with transition metal complexes featuring thermally activated delayed fluorescence (TADF) mechanism. First, the TADF mechanism is briefly introduced, as well as the experimental and theoretical methods applied to study TADF in transition metal complexes. Second, the review presents an exhaustive overview of OLED and LEC devices incorporating organometallic TADF emitters. For each type of device, the description of TADF is organized by respective elements focusing on each emission color, that is, blue, green/yellow, orange/red and, if existing, white. Finally, insights and future potential development of organometallic TADF emitters for lighting devices are comprehensively discussed. Overall, this review complements recent ones focused on TADF small molecules applied to the SSLD field., This work was supported by the “Ministère de la Recherche et des Nouvelles Technologies,” CNRS (Centre National de la Recherche Scientifique), and the LABEX SynOrg (ANR‐11‐LABX‐0029). The authors thank Normandie University (G.U.M.) for funding. R.D.C. acknowledges the program “Ayudas para la atracción de talento investigador – Modalidad 1 of the Consejería de Educación, Juventud y Deporte—Comunidad de Madrid with the reference number 2016‐T1/IND‐1463.” R.D.C. acknowledges Spanish MINECO for the Ramón y Cajal program (RYC‐2016‐20891), the Europa Excelencia program (ERC2019‐092825), the 2018 Leonardo Grant for Researchers and Cultural Creators from BBVA Foundation, and FOTOART‐CM project funded by Madrid region under programme P2018/NMT‐4367. J.F.‐C. acknowledges the Marie Skłodowska‐Curie Individual Fellowships (H2020‐MSCA‐IF‐2017).

Published
2020

5. Cytotoxicity of cationic NHC copper(I) complexes coordinated to 2,2'-bis-pyridyl ligands

Author

Richard Daniellou, Eric Duverger, Sylvain Gaillard, Jean-Luc Renaud, Margaux Elie, Gilbert Umuhire Mahoro, Laboratoire de chimie moléculaire et thioorganique (LCMT), Centre National de la Recherche Scientifique (CNRS)-Institut Normand de Chimie Moléculaire Médicinale et Macromoléculaire (INC3M), Institut de Chimie du CNRS (INC)-École Nationale Supérieure d'Ingénieurs de Caen (ENSICAEN), Normandie Université (NU)-Normandie Université (NU)-Institut national des sciences appliquées Rouen Normandie (INSA Rouen Normandie), Institut National des Sciences Appliquées (INSA)-Normandie Université (NU)-Institut National des Sciences Appliquées (INSA)-Université Le Havre Normandie (ULH), Normandie Université (NU)-Université de Rouen Normandie (UNIROUEN), Normandie Université (NU)-Centre National de la Recherche Scientifique (CNRS)-Université de Caen Normandie (UNICAEN), Normandie Université (NU)-Institut de Chimie du CNRS (INC)-École Nationale Supérieure d'Ingénieurs de Caen (ENSICAEN), Normandie Université (NU), Institut de Chimie Organique et Analytique (ICOA), Université d'Orléans (UO)-Centre National de la Recherche Scientifique (CNRS)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Institut de Chimie du CNRS (INC)-Institut National de la Santé et de la Recherche Médicale (INSERM), Université de Caen Normandie (UNICAEN), Normandie Université (NU)-Normandie Université (NU)-École Nationale Supérieure d'Ingénieurs de Caen (ENSICAEN), Normandie Université (NU)-Institut Normand de Chimie Moléculaire Médicinale et Macromoléculaire (INC3M), Normandie Université (NU)-Université Le Havre Normandie (ULH), Normandie Université (NU)-Institut national des sciences appliquées Rouen Normandie (INSA Rouen Normandie), Institut National des Sciences Appliquées (INSA)-Normandie Université (NU)-Institut National des Sciences Appliquées (INSA)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université Le Havre Normandie (ULH), Institut National des Sciences Appliquées (INSA)-Normandie Université (NU)-Institut National des Sciences Appliquées (INSA)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS), Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université d'Orléans (UO)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), and CCSD, Accord Elsevier

Subjects
NHC, Cytotoxicity, chemistry.chemical_element, 010402 general chemistry, 01 natural sciences, Biochemistry, Inorganic Chemistry, Nitrogen ligand, Materials Chemistry, Physical and Theoretical Chemistry, Cancer, [CHIM.MATE] Chemical Sciences/Material chemistry, 010405 organic chemistry, Chemistry, [CHIM.ORGA]Chemical Sciences/Organic chemistry, Organic Chemistry, Cationic polymerization, [CHIM.CATA] Chemical Sciences/Catalysis, [CHIM.CATA]Chemical Sciences/Catalysis, [CHIM.MATE]Chemical Sciences/Material chemistry, Prodrug, [CHIM.ORGA] Chemical Sciences/Organic chemistry, Combinatorial chemistry, Copper, 0104 chemical sciences, 3. Good health, Cancer cell lines
Abstract

International audience; Cytotoxicity of cationic (NHC)Cu(I) complexes bearing 2,2′-dipyridylamine (dpa) type ligands has been evaluated toward 4 cancer cell lines, and compared to the one of neutral (NHC)Cu(I) complexes. The high cytotoxicity of these novel cationic (NHC)Cu(I) complexes, combined with the straightforward synthesis, and versatility of dpa type ligands may offer new prospects in cancer research, toward the development of novel carrier linked prodrugs.

Published
2019
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6. Continuous flow ring-closing metathesis, an environmentally-friendly route to 2,5-dihydro-1H-pyrrole-3-carboxylates

Author

Marcin Drop, Gilles Subra, Paweł Zajdel, Maciej Pawłowski, Jean Martinez, Katarzyna Grychowska, Xavier Bantreil, Evelina Colacino, Frédéric Lamaty, Gilbert Umuhire Mahoro, Department of Medicinal Chemistry, Uniwersytet Jagielloński w Krakowie = Jagiellonian University (UJ), Institut des Biomolécules Max Mousseron [Pôle Chimie Balard] (IBMM), and 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)

Subjects
Diene, 010405 organic chemistry, Chemistry, [CHIM.ORGA]Chemical Sciences/Organic chemistry, [CHIM.CATA]Chemical Sciences/Catalysis, 010402 general chemistry, Residence time (fluid dynamics), Metathesis, 01 natural sciences, Pollution, Environmentally friendly, 0104 chemical sciences, Solvent, chemistry.chemical_compound, Ring-closing metathesis, Environmental Chemistry, Organic chemistry, [CHIM]Chemical Sciences, Dimethyl carbonate, Pyrrole
Abstract

International audience; 2,5-Dihydro-1H-pyrrole-3-carboxylates are important building blocks for the synthesis of high value pyrroles and pyrroloquinoline derivatives with interesting biological activities. The use of continuous flow allowed us to perform a key synthetic step, namely ruthenium-catalyzed ring-closing metathesis, with a residence time of 1 min at 120°C. Dimethyl carbonate, a green solvent, was demonstrated for the first time to be an excellent solvent for this reaction in continuous flow. The continuous flow conditions proved to be general and the scale-up of this reaction was not only possible, but also highly efficient. Conversion of 10 grams of diene was realized in 37 minutes under continuous flow, yielding the desired heterocycle in 91% yield. Fig. 1 Pharmaceutical drugs synthesized using olefin metathesis. † Electronic supplementary information (ESI) available. See

Published
2017
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