Synthesis and Antitubercular Activity of a Series of Thiazole Derivatives

Author(s): Mahesh Chhabria, Shailesh Patel, Sandeep Dholakia, Hardik Mistry, Sweta Patel.

Journal Name: Anti-Infective Agents

Volume 12 , Issue 2 , 2014

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Abstract:

Tuberculosis (TB) is of increasing concern due to the recent emergence and spread of MDR-TB, XDR-TB, TDR-TB and HIV/AIDS pandemic. There is urgent need for novel antitubercular agents which can shorten the treatment duration. Based on isosteric replacement and 3D structural similarity between Linezolid, an oxazolidine antimycobacterial agent, we have designed novel 4-amino-3,5-di(substituted)thiazolin-2(3H)thione/ones, synthesized and evaluated for their antimycobacterial activity on Mycobacterium tuberculosis H37Rv strain. Some of the compounds exhibited potent antimycobacterial activity with MIC values in the range of 1-2 µg/mL. Active compounds were further screened against MDR-TB and XDR-TB strain and found to exhibit promising in vitro activity.

Keywords: Antimycobacterial activity, MDR-TB, thiazolin-thione/ones, XDR-TB.

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Article Details

VOLUME: 12
ISSUE: 2
Year: 2014
Page: [149 - 158]
Pages: 10
DOI: 10.2174/22113525113119990119
Price: $58

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