Abstract

DESIGN AND CHARACTERISATION OF NOVEL 1, 5-BENZOTHIAZEPINES BY HETEROARYL CYCLIZATION AND BIOLOGICAL SCREENING FOR ANTIMICROBIAL ACTIVITY

Kumara Prasad S. A.*, Chethan S. H. and Shabaraya A. R.

ABSTRACT

A new series of 1, 5-benzothiazepine derivatives are synthesised by the reaction of various chalcones of 2-acetylpyrazine with 2-aminothiophenol via heteroaryl cyclization. Melting points of the synthesized compounds were determined by open capillary and are uncorrected. The purity of the compounds was checked using precoated TLC plates (60F) using chloroform: methanol (8:2) solvent system. The developed chromatographic plates were visualized under UV at 254nm. IR spectra were recorded using KBr on Josco FTIR model 8400 spectrophotometer, 1H NMR spectra in DMSO on a BRUKER FT-NMR instrument using TMS as internal standard. The designed compounds were screened for Antibacterial activity against Gram-positive (S. aureus and B. Subtilis) and Gram-negative (S. typhi and E. coli) bacteria and Antifungal activity against against A. Niger and C. Albicans in comparison with Ofloxacin and Fluconazole as standard to reveal the potency of synthesized derivatives. In accordance with the data obtained from antimicrobial activity, all the synthesized compounds have shown good activity against the tested microbes.

Keywords: Chalcones, 1, 5-benzothiazepines, antimicrobial activity.