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Synthesis and Biological Evaluation of 2-thiazolylimino-5-arylidene-4- thiazolidinone Derivatives as Potent Antimycobacterial Agents

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Background: The recent emergence of multi-drug resistant (MDR) and extensively drugresistant (XDR) cases of tuberculosis has lead to the search for new structural classes of anti-TB drugs that can be effective against these strains of Mycobacterium tuberculosis. In the present study a series of 2-thiazolylimino-5-arylidene-4-thiazolidinone derivatives, unsubstituted and mono-substituted with hydroxy, methoxy, fluoro, chloro and nitro groups on the aryl ring were synthesized and assayed for their in vitro antimycobacterial activity against drug-sensitive M. tb H37Rv strain. Methods: In vitro antimycobacterial activity against drug-sensitive M. tb H37Rv strain (susceptible both to rifampicin and isoniazid) was performed and expressed as % inhibition at minimum inhibitory concentration (MIC) values. Compounds were initially tested for IC99 at a concentration of 6.25 μg/ml in BACTEC-460 TB radiometric system, and Isoniazid (0.1 μg/ml) and rifampicin (2.0 μg/ml) were taken as reference standards. Results: We report the synthesis and antimycobacterial activities of 2- thiazolylimino-5-arylidene-4-thiazolidinone derivatives, expressed as % inhibitions, and their MIC values. All of the above synthesized compounds showed substantial antimycobacterial activity in the preliminary screening, and some of the compounds, 8-14, exhibited excellent antimycobacterial activities (86-98 % inhibition) at 6.25–12.5 μg/ml against drugsensitive M. tb H37Rv strain. Conclusion: The 2-thiazolylimino-5-arylidene-4-thiazolidinone derivatives were identified as a new antitubercular chemical entity in this study. Two of the active compounds, 9 and 14 and their derivatives have been identified as potential lead molecules for further drug development. It was observed that the hydroxyl and bulky alkoxy groups enhance antimycobacterial activity, while a halogen substituent decreases the activity. Further structural optimization and identification of molecules are underway in our laboratory..
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Keywords: Antimycobacterial activity; Mycobacterium tuberculosis; Thiazolidinone derivatives

Document Type: Research Article

Publication date: August 1, 2015

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  • Anti-Infective Agents publishes original research, expert reviews, drug clinical trial studies and guest edited issues on all the latest and outstanding developments on the medicinal chemistry, biology, pharmacology and use of anti-infective and anti-parasitic agents. The scope of the journal covers all pre-clinical and clinical research on antimicrobials, antibacterials, antiviral, antifungal, and antiparasitic agents. Anti-Infective Agents is an essential journal for all infectious disease researchers in industry, academia and the health services.
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