Abstract
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.
Anti-Infective Agents
Title:Molecular Hybridization and Preclinical Evaluation of Imines From Para-substituted 4-phenyl 2-amino Thiazole Incorporated with Isatin Analogues as Antitubercular Agents
Volume: 13 Issue: 1
Author(s): Nice Joy and Bijo Mathew
Affiliation:
Keywords: Analogues, antitubercular agents, isatin, mycobacteria, molecular hybridization, thiazole.
Abstract: 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.
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Joy Nice and Mathew Bijo, Molecular Hybridization and Preclinical Evaluation of Imines From Para-substituted 4-phenyl 2-amino Thiazole Incorporated with Isatin Analogues as Antitubercular Agents, Anti-Infective Agents 2015; 13 (1) . https://dx.doi.org/10.2174/2211352512666140905232639
DOI https://dx.doi.org/10.2174/2211352512666140905232639 |
Print ISSN 2211-3525 |
Publisher Name Bentham Science Publisher |
Online ISSN 2211-3533 |
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