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ISSN 2063-5346
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Synthesis and Evaluation of Novel Heterocycles as Anti-Tubercular Agents

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K Gokul, C Sridaran, Satyajit Barik, M K Kathiravan, D Priya*
» doi: 10.48047/ecb/2023.12.10.148

Abstract

Tuberculosis, an infectious disease, has been reported to cause 1.5 million death in 2020 and the possibility is more among people with HIV. The continuous global spread of tuberculosis is mostly due to multi-drug-resistant tuberculosis. Drug resistance generated against mutant Mycobacterium tuberculosis strains poses a problem for drug development in identifying new molecules or compounds to treat the evolved resistant strains. Mimicking the vital mycobacterial cell wall component fatty acid, mycolic acids the present study aims to design and synthesize a series of Pyrazole derivatives through molecular hybridization approach which are proposed to block mycobacterial cell wall biosynthetic pathway (FAS II) by inhibiting InhA enzyme. Hence, in this study, we have focussed on the synthesis of pyrazole, oxo-pyrimidine derivatives from chalcone derivatives synthesised through cyclo-condensation with hydrazine hydrate and urea, respectively and evaluated for their anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain by Microplate Alamar Blue assay (MABA) method. Among the synthesised pyrazole derivatives, compound 4 with bromo phenyl and tolyl substitution showed excellent anti-tubercular activity when compared with the oxo-pyrimidine derivatives with MIC 3.12μg/ml.

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