- Design, synthesis and biological evaluation of imidazo[2,1-b]thiazole and benzo[d]imidazo[2,1-b]thiazole derivatives as Mycobacterium tuberculosis pantothenate synthetase inhibitors
-
In the present study, we have designed imidazo[2,1-b]thiazole and benzo[d]imidazo[2,1-b]thiazole derivatives from earlier reported imidazo[1,2-a]pyridine based Mycobacterium tuberculosis (MTB) pantothenate synthetase (PS) inhibitors. We synthesized thirty compounds and they were evaluated for MTB PS inhibition study, in vitro anti-TB activities against replicative and non-replicative MTB, in vivo activity using Mycobacterium marinum infected Zebra fish and cytotoxicity against RAW 264.7 cell line. Among them compound 2-methyl-N′-(4-phenoxybenzoyl)benzo[d]imidazo[2,1-b]thiazole-3-carbohydrazide (5bc) emerged as potent compound active against MTB PS with IC50 of 0.53 ± 0.13 μM, MIC of 3.53 μM, 2.1 log reduction against nutrient starved MTB, with 33% cytotoxicity at 50 μM. It also showed 1.5 log reduction of M. marinum load in Zebra fish at 10 mg/kg.
- Samala, Ganesh,Devi, Parthiban Brindha,Saxena, Shalini,Meda, Nikhila,Yogeeswari, Perumal,Sriram, Dharmarajan
-
p. 1298 - 1307
(2016/03/01)
-
- Fused heterocycles: Synthesis of some new imidazothiazoles
-
Reaction of aldehyde-hydrazones or semicarbazones bearing an imidazo[2,1-b] [1,3] thiazole ring system with mercaptoalkanoic acids were investigated. Antimycobacterial activities of compounds thus obtained were evaluated against Mycobacterium tuberculosis H37Rv using rifampine as standard.
- Cesur, Nesrin,Cesur, Zafer,Guner, Handan,Kasimogullari, B. Ozden
-
p. 433 - 438
(2007/10/03)
-