Novel fatty acid-thiadiazole derivatives as potential antimycobacterial agents.

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ID: 64099
2019
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Abstract
The discovery of antibiotics around the middle twentieth century led to a decrease in the interest in antimycobacterial fatty acids. In order to re-establish the importance of naturally abundant fatty acid, a series of fatty acid-thiadiazole derivatives were designed and synthesized based on molecular hybridization approach. In vitro antimycobacterial potential was established by a screening of synthesized compounds against Mycobacterium tuberculosis H37Rv strain. Among them, compounds 5a, 5d, 5h, and 5j were the most active, with compound 5j exhibiting minimum inhibitory concentration of 2.34 μg/ml against M.tb H37Rv. Additionally, the compounds were docked to determine the probable binding interactions and understand the mechanism of action of most active molecules on enoyl-acyl carrier protein reductases (InhA), which is involved in the mycobacterium fatty acid biosynthetic pathway.
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mali2019novelchemical Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Mali, Jaishree K;Sutar, Yogesh B;Pahelkar, Akshata R;Verma, Preeti M;Telvekar, Vikas N;
Journal Chemical biology & drug design
Year 2019
DOI
10.1111/cbdd.13634
URL
Keywords
Docking fatty acid mycobacterium tuberculosis resazurin microtiter assay thiadiazole

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