Synthesis, In-vitro and In-silico Studies of Benzothiazole Azo-Ester Derivatives as Anti-TB Agents

(E-pub Ahead of Print)

Author(s): Mahesh Bhat*, Belagali S. L..

Journal Name: Anti-Infective Agents

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Introduction: A new series of benzothiazole azo-ester derivatives was synthesized by using Steglish esterification reaction.

Methods: All the synthesized compounds were screened for their anti-TB activities by in-vitro microplate Alamar Blue assay method against M. tuberculosis (H37RV strain). All the compounds showed activities and their MIC values were over the range of 1.6 μg/mL to 50 μg/mL. The compounds 4d and 4j showed superior activity with MIC 1.6 μg/mL compared to the standard drug Streptomycin (MIC 6.25 μg/mL), Pyrazinamide (MIC 3.125 μg/mL) and Ciprofloxacin (MIC 3.125 μg/mL). Molecular docking study was carried out with enoyl acyl carrier reductase (InhA) of M. tuberculosis and decaprenyl phosphoryl-D-ribose oxidase (DprE1).

Results: These studies showed that these compounds have more interaction with InhA protein whereas some compounds could not be docked into DprE1.

Keywords: Azo-ester, anti-TB, Molecular docking, esterification

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(E-pub Ahead of Print)
DOI: 10.2174/2211352517666190126160534

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