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Your search keyword '"Mahama Ouattara"' showing total 7 results
Start Over Author "Mahama Ouattara" Topic drug discovery
7 results on '"Mahama Ouattara"'

1. Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis

Author

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)

Subjects
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.

Published
2020
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2. Discovery of imidazo[1,2-a]pyridine-based anthelmintic targeting cholinergic receptors of Haemonchus Contortus

Author

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

Subjects
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.

Published
2017
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3. Exploration of potential prodrug approach of the bis-thiazolium salts T3 and T4 for orally delivered antimalarials

Author

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
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4. Disulfide prodrugs of albitiazolium (T3/SAR97276): synthesis and biological activities

Author

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
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5. Design and synthesis of amidoxime derivatives for orally potent C-alkylamidine-based antimalarial agents

Author

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
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6. Potent antimalarial activity of 2-aminopyridinium salts, amidines, and guanidines

Author

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
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7. Synthesis and antimalarial activity of new 1,12-bis(N,N'-acetamidinyl)dodecane derivatives

Author

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
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