Abstract
SHS investigation development is considered from the geographical and historical viewpoint. 3 stages are described. Within Stage 1 the work was carried out in the Department of the Institute of Chemical Physics in Chernogolovka where the scientific discovery had been made. At Stage 2 the interest to SHS arose in different cities and towns of the former USSR. Within Stage 3 SHS entered the international scene. Now SHS processes and products are being studied in more than 50 countries.
Abstract
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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Authors:Bentham Science Books