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Synthesis of some novel piperidine fused 5-thioxo-1H-1,2,4-triazoles as potential antimicrobial and antitubercular agents

A novel series of analogues based on 5-(1-(4-chloro-3-methoxyphenyl)piperidin-4-yl)-4-phenyl-2 H -1,2,4-triazole-3(4 H )-thione core have been synthesized and their potential as antibacterial, antifungal and antitubercular agents was examined. The structure-activity relationship (SAR) studies of the...

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Published in:Journal of chemical sciences (Bangalore, India) India), 2021, Vol.133 (1), Article 3
Main Authors: RISHIKESAN, R, KARUVALAM, RANJITH P, MUTHIPEEDIKA, NIBIN JOY, SAJITH, AYYILIATH M, EEDA, KOTI REDDY, PAKKATH, RAJEESH, HARIDAS, KARICKAL R, BHASKAR, VAISHNAV, NARASIMHAMURTHY, KEREYAGALAHALLY H, MURALIDHARAN, A
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Language:English
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Summary:A novel series of analogues based on 5-(1-(4-chloro-3-methoxyphenyl)piperidin-4-yl)-4-phenyl-2 H -1,2,4-triazole-3(4 H )-thione core have been synthesized and their potential as antibacterial, antifungal and antitubercular agents was examined. The structure-activity relationship (SAR) studies of these derivatives 5 ( a–k ) clearly indicate the vital role of lipophilicity as a major factor in enhancing the biological activity of these compounds. Among the compounds screened, 5a , 5c , 5d , 5j and 5k displayed significant activity against Mycobacterium tuberculosis H37Rv strain. Graphic abstract
ISSN:0974-3626
0973-7103
DOI:10.1007/s12039-020-01872-4