Bioorganic and Medicinal Chemistry p. 1298 - 1307 (2016)
Update date:2022-08-04
Topics:
Samala, Ganesh
Devi, Parthiban Brindha
Saxena, Shalini
Meda, Nikhila
Yogeeswari, Perumal
Sriram, Dharmarajan
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.
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Doi:10.1021/ja01167a058
(1950)Doi:10.1055/s-2003-41042
(2003)Doi:10.1016/0040-4020(72)88157-2
(1972)Doi:10.1016/S0022-1139(00)82155-7
(1977)Doi:10.1021/ja00450a048
(1977)Doi:10.1007/BF01156478
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