In-Silico and In-Vitro Approaches to Screen the Antituberculosis Activity of Benzothiazole Analogs

Synthesis and Anti-TB Activity Screening of Benzothiazole Amide Derivatives

Author(s): Mahesh Bhat and S.L. Belagali

Pp: 66-76 (11)

DOI: 10.2174/9789811494635121010007

* (Excluding Mailing and Handling)


Synthesis of diamide derivatives are carried out by the phenylalanine initially phenylalanine reacts with the aromatic amine by the acid amine coupling followed by de-protection of the boc and further reacts with the benzothiazole carboxylic acid by the formation of the amide coupling in the presence HATU as coupling reagent. Further series of the diamide benzothiazole derivative compounds were screened for the in-silico and in-vitro anti TB activity. In in-silico method compounds show a good docking score with respect to the standard drug. In-vitro Alamar blue assay demonstrate some of the compounds marked for the superior activity with minimum inhibitory concentration 1.6 μg/mL.

Keywords: Alamar Blue Assay, Amide, Anti-TB, Benzothiazole, Boc, Diethyl oxalate, DIPEA, Docking, DprE1, HATU, InhA, Isoniazid, MIC, Phenyl alanine, Pyrazinamide, T3P, Trifluoro acetic acid, Triethylamine, Tuberculosis.

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