SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF SOME NOVEL BENZOTHIAZOLE ANALOGS AS POTENTIAL ANTITUBERCULAR AGENTSAbstract
Benzthiazole, Chalcones, and their analogs have a wide variety of biological activities like antihelminthic, antifungal, antibacterial, anti-diabetic, anti-tubercular, anti-inflammatory, anticonvulsant, diuretic etc., In the present research work, an effort has been made to synthesize some new series of novel benzothiazole linked chalcones from 3-amino-acetophenone and potassium thiocyanate which were dissolved in glacial acetic acid at room temperature. Liquid bromine in glacial acetic acid was then added drop-wise, and finally, the reaction mass is quenched and basified with ammonia to obtain the desired Benzthiazole linked chalcone. The progress of the reaction is monitored through TLC. The purity of the compounds was identified by TLC and purified by recrystallization and column chromatography. The structures were determined by IR, 1H NMR, and Mass spectral data. The synthesized benthiazole linked chalcone analogues were screened for anti-tubercular activity by the use of MABA (Microplate Alamar Blue assay) analytical method on H37Rv strain of Mycobacterium tuberculosis. Based on the results of anti-tubercular activity, it can be seen that the compounds containing electron-withdrawing groups like chlorine, fluorine, nitrogen showed better activity than that of the other compounds in the series. The mechanism of action of the compounds can assassinate for their cell wall disruption by inhibiting the peptidoglycan synthesis as a potential antimicrobial agent or inhibiting the synthesis of mycolic acid as a potential anti-tubercular agent.
S. A. Satyadev *, R. K. Prava, S. Mantha, A. Koduru and T. Gowtami
A. U. College of Pharmaceutical Sciences, Andhra University, Visakhapatnam, Andhra Pradesh, India.
12 January 2020
09 March 2020
11 March 2020
01 January 2021