SYNTHESIS, CHARACTERISATION, AND IN VITRO BIOLOGICAL EVALUATION OF A SERIES OF NOVEL BENZOTHIAZOLE DERIVATIVES AS ANTIBACTERIAL AGENTS

Abstract

A group of benzothiazole-amide derivatives (VH01-06) were conventionally synthesised in using modified reaction conditions of the Schotten-Baumann named reaction, all the synthesised compounds were characterised using physical methods such as Thin-layer chromatography to determine the retention factor and melting point. All the chemical structure of the compounds were consistently with the spectral data obtained for FT-IR, 1H & 13C NMR and HRMS ESI-Mass spectroscopic techniques. These compounds were further exposed to in vitro antibacterial activity screening various strains includes gram-positive bacteria (Methicillin-resistant Staphylococcus aureus (MRSA) ATCC 3359 and Methicillinsensitive Staphylococcus aureus (MSSA) ATCC 2592 and gram-negative bacteria (Escherichia coli J53 R1, Escherichia coli ATCC 25922, Klebsiella pneumoniae ATCC 10031 and Klebsiella pneumonia BAA-1075). Based on the screening results, the benzothiazole compounds were appeared to be active at 100μM concentration. However, one compound was reported as active against E. coli ATCC 25923 at 200 μg/mL. Keywords: Benzothiazole, in vitro antibacterial activity.