Synthesis and biological evaluation of some benzothiazole-2-thiol derivatives as potent quorum sensing inhibitors

Abstract

QS is a well-known mechanism of bacteria cell-to-cell communication. By inhibiting the quorum sensing pathway, compounds can prevent the aggressive activity of bacteria, including virulence production, biofilm formation, and other pathogenesis. Herein, the authors reported the synthesis and biological evaluation of several benzothiazole-2-thiols toward quorum sensing activities. As a result, five compounds are successfully synthesised using microwave methodology in good yields. In terms of bioactivity, compounds 2, 5 showed moderated quorum sensing inhibitory activity with IC₅₀ of 212.03±2.17 and 198.11±3.48 µg/ml, respectively, in comparison to that of reference compound 4NPO. This research provides a novel template for future drug discovery and development.