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Start Over Author "Bazin MA" Topic antiprotozoal agents
3 results on '"Bazin MA"'

1. Synthesis, antileishmanial activity and cytotoxicity of 2,3-diaryl- and 2,3,8-trisubstituted imidazo[1,2-a]pyrazines.

Author

Marchand P, Bazin MA, Pagniez F, Rivière G, Bodero L, Marhadour S, Nourrisson MR, Picot C, Ruchaud S, Bach S, Baratte B, Sauvain M, Pareja DC, Vaisberg AJ, and Le Pape P

Subjects
Animals, Antiprotozoal Agents chemical synthesis, Antiprotozoal Agents chemistry, Cell Line, Cell Proliferation drug effects, Dose-Response Relationship, Drug, Humans, Imidazoles chemical synthesis, Imidazoles chemistry, Mice, Mice, Inbred BALB C, Molecular Structure, Pyrazines chemical synthesis, Pyrazines chemistry, Structure-Activity Relationship, Antiprotozoal Agents pharmacology, Fibroblasts drug effects, Imidazoles pharmacology, Leishmania major drug effects, Macrophages drug effects, Pyrazines pharmacology
Abstract

A series of original 2-phenyl-3-(pyridin-4-yl)imidazo[1,2-a]pyrazines and the 3-iodo precursors, bearing a polar moiety at the C-8 position, was synthesized and evaluated for their antileishmanial activities. Two derivatives exhibited very good activity against the promastigote and the amastigote forms of Leishmania major in the micromolar to submicromolar ranges, coupled with a low cytotoxicity against macrophages and 3T3 mouse fibroblast cells. Through LmCK1 inhibition assay, investigations of the putative molecular target of these promising antileishmanial compounds will be discussed., (Copyright © 2015 Elsevier Masson SAS. All rights reserved.)

Published
2015
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2. Synthesis and biological evaluation of 2,3-diarylimidazo[1,2-a]pyridines as antileishmanial agents.

Author

Marhadour S, Marchand P, Pagniez F, Bazin MA, Picot C, Lozach O, Ruchaud S, Antoine M, Meijer L, Rachidi N, and Le Pape P

Subjects
Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Antiprotozoal Agents chemical synthesis, Antiprotozoal Agents chemistry, Casein Kinase I antagonists & inhibitors, Casein Kinase I metabolism, Cell Proliferation drug effects, Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, HeLa Cells, Humans, Leishmania major enzymology, Models, Molecular, Molecular Structure, Parasitic Sensitivity Tests, Protein Kinase C antagonists & inhibitors, Protein Kinase C metabolism, Protein Kinase Inhibitors chemical synthesis, Protein Kinase Inhibitors chemistry, Pyridines chemical synthesis, Pyridines chemistry, Structure-Activity Relationship, Antineoplastic Agents pharmacology, Antiprotozoal Agents pharmacology, Leishmania major drug effects, Protein Kinase Inhibitors pharmacology, Pyridines pharmacology
Abstract

A novel series of 2,3-diarylimidazo[1,2-a]pyridines was synthesized and evaluated for their antileishmanial activities. Four derivatives exhibited good activity against the promastigote and intracellular amastigote stages of Leishmania major, coupled with a low cytotoxicity against the HeLa human cell line. The impact of compound lipophilicity on antiparasitic activities was investigated by Log D comparison. Although LmCK1 could be the parasitic target for three compounds (13, 18, 21), the inhibition of another target is under study to explain the antileishmanial effect of the most promising compounds., (Copyright © 2012 Elsevier Masson SAS. All rights reserved.)

Published
2012
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3. Synthesis of oxysterols and nitrogenous sterols with antileishmanial and trypanocidal activities.

Author

Bazin MA, Loiseau PM, Bories C, Letourneux Y, Rault S, and El Kihel L

Subjects
Animals, Cells, Cultured, Female, Leishmania donovani classification, Macrophages parasitology, Mice, Molecular Structure, Parasitic Sensitivity Tests, Stereoisomerism, Structure-Activity Relationship, Antiprotozoal Agents chemical synthesis, Antiprotozoal Agents chemistry, Antiprotozoal Agents pharmacology, Leishmania donovani drug effects, Steroids chemical synthesis, Steroids chemistry, Steroids pharmacology, Trypanocidal Agents chemical synthesis, Trypanocidal Agents chemistry, Trypanocidal Agents pharmacology, Trypanosoma brucei brucei drug effects
Abstract

Two sterol families have been synthesized: the first one is nitrogenous sterols containing amino, N-hydroxyimino or cyano group and the second one is oxysterols such as ketosterol and hydroxysterols. These compounds were then evaluated in vitro against Leishmania donovani promastigotes and Trypanosoma brucei brucei trypomastigotes. The most active compounds against L. donovani promastigotes were 7beta-aminomethylcholesterol and 7alpha,beta-aminocholesterol (IC50 in a range from 1 to 3 microM, pentamidine: 2.8 microM). These compounds were active on intramacrophage amastigotes with IC50 of 1.3 microM. Such an activity justifies further in vivo antileishmanial evaluation. Against T. b. brucei, (24R,S)-24-hydroxy-24-methylcholesterol (MEC, 12.5 microM) was the most active compound from these series.

Published
2006
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