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

ISSN: 2211-3533 (Online)
ISSN: 2211-3525 (Print)


Volume 14, 2 Issues, 2016


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Anti-Infective Agents

Formerly: Anti-Infective Agents in Medicinal Chemistry

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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, 13(1): 60-64.

Author(s): Nice Joy and Bijo Mathew.

Affiliation: Division of Drug Design and Medicinal, Chemistry Research Lab, Department of Pharmaceutical Chemistry, Grace College of Pharmacy, Palakkad-678004, Kerala, India.

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.



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Article Details

Volume: 13
Issue Number: 1
First Page: 60
Last Page: 64
Page Count: 5
DOI: 10.2174/2211352512666140905232639
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