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.
