European Journal of Biomedical and Pharmaceutical Sciences

MICROWAVE ASSISTED SYNTHESIS OF BENZOCOUMARIN-BENZOTHIAZEPINE HYBRIDS AS POTENT ANTI-TUBERCULAR AGENTS AND THEIR DNA CLEAVAGE STUDY

Kallappa. M. Hosamani* Dinesh S. Reddy and Kanchugarakoppal S. Rangappa

ABSTRACT

An efficient and expeditious method has been developed for the synthesis of benzocoumarin-benzothiazepine hybrids, under microwave irradiation. The present methodology is cost-effective in addition to other advantages like mild reaction condition, high yields of products in shorter reaction time and simple workup procedure. The structure of all the newly synthesized compounds was confirmed by elemental and spectroscopic analyses. All the newly synthesized
compounds (2a-2j) were evaluated for their in-vitro antitubercular and DNA cleavage study. Among all the screened compounds, (2h) showed most pronounced activity against Mycobacterium tuberculosis (Mtb) obtaining MIC of 3.12 μg/mL. The compounds were further subjected for DNA cleavage study by agarose gel electrophoresis method, which revealed that compound (2h) inhibits the growth of the pathogenic organism by cleaving the genome as no traces of DNA were found.

Keywords: Coumarin, Benzothiazepine, Microwave synthesis, Anti-tuberculosis and DNA cleavage studies.