Design, synthesis and anti-mycobacterial activity evaluation of benzofuran-isatin hybrids

A series of novel benzofuran-isatin hybrids were designed, synthesized and evaluated for their in vitro anti-mycobacterial activities as well as cytotoxicity. Preliminary results indicated that all hybrids with acceptable cytotoxicity in VERO cells exhibited considerable anti-mycobacterial activities against MTB H37Rv and MDR-TB strains. It is worth noting that hybrid 8f with no cytotoxicity towards VERO cells, was found to be the most active compound against MTB H37Rv and MDR-TB. Comparing to the first-line anti-TB agents (rifampicin and isoniazid), hybrid 8f was more active against MDR-TB. However, both the metabolic stability and in vivo pharmacokinetic profiles of 8f were inferior to inhibitor TAM16. Further modification based on hybrid 8f is needed to improve metabolic stability and pharmacokinetic profiles.204