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Synthesis, In-Vitro and In-Silico Studies of Benzothiazole Azo-Ester Derivatives as Anti-TB Agents

[ Vol. 18 , Issue. 1 ]

Author(s):

Mahesh Bhat* and Shiddappa L. Belagali   Pages 15 - 23 ( 9 )

Abstract:


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 µ g/mL), Pyrazinamide (MIC 3.125 µ g/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 and Conclusion: 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, ciprofloxacin, steglish esterification reaction.

Affiliation:

Department of Chemistry, Bangurnagar Arts, Science and Commerce College, Dandeli - 581 325 Karnataka, Environmental Chemistry Laboratory, Department of Studies in Environmental Science, University of Mysore, Manasagangothri, Mysore -570 006, Karnataka

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