Molecular Hybridization and Preclinical Evaluation of Imines From Para-substituted 4-phenyl 2-amino Thiazole Incorporated with Isatin Analogues as Antitubercular Agents

Author(s): Nice Joy, Bijo Mathew.

Journal Name: Anti-Infective Agents
Anti-Infective Agents in Medicinal Chemistry

Volume 13 , Issue 1 , 2015

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A series of isatin imines incorporated with 4-sustituted phenyl 2-amino thiazole was synthesized on the basis of molecular hybridization drug design principle. The structures of the derivatives were confirmed by IR, 1HNMR and Mass analyses. The titled derivatives were screened against M.tuberculosis strain H37RVusing alamar blue susceptibility test. Compound 3-{[4-(4- hydroxyphenyl)-1, 3-thiazol-2-yl] imino}-1, 3-dihydro-2H-indol-2-one (IIT2) was found to be most active with a MIC of 6.25µg/ml. Preclinical evaluation of the compounds was ascertained by in silico toxicity and ADME parameters. It has been concluded that the hydrogen contributing groups present in the phenyl system of the titled scaffold favours the activity ratio.

Keywords: Analogues, antitubercular agents, isatin, mycobacteria, molecular hybridization, thiazole.

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Article Details

Year: 2015
Page: [60 - 64]
Pages: 5
DOI: 10.2174/2211352512666140905232639

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PDF: 36
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