DESIGN, SYNTHESIS AND IN VITRO ANTI-BACTERIAL ACTIVITIES OF BENZOFURAN-ISATIN HYBRIDS

A series of novel benzofuran-isatin hybrids 6a-x tethered through propylene, butylene, pentylene and hexylene were designed, synthesized and evaluated for their in vitro anti-bacterial activities against a panel of clinically important Gram-positive and Gram-negative pathogens including drug-resistant bacteria. All hybrids exhibited decent in vitro anti-bacterial activities, and the most active hybrid 6l was not only comparable to vancomycin against the majority of the tested Gram-positive strains, but also highly active against Gram-negative bacteria. Based on the above results, hybrid 6l could act as a lead for further investigation. Moreover, the enriched structure-activity relationship may pave the way for further optimization.