Bioorganic & Medicinal Chemistry 2007-03-01

Synthesis and antimycobacterial evaluation of benzofurobenzopyran analogues.

Soizic Prado, Yves L Janin, Brigitte Saint-Joanis, Priscille Brodin, Sylvie Michel, Michel Koch, Stewart T Cole, François Tillequin, Pierre-Etienne Bost

Index: Bioorg. Med. Chem. 15 , 2177-86, (2007)

Full Text: HTML

Abstract

We recently reported that 3,3-dimethyl-3H-benzofuro[3,2,f][1]-benzopyran and its hydrogenated analogue are selective in vitro inhibitors of mycobacterial growth. However, their lack of in vivo activity on a murine model of Mycobacterium tuberculosis infection due to their poor bioavailability led to a structure-activity relationship investigation. We wish to report here the preparation of some structural analogues along with their biological effect on the growth of Mycobacterium smegmatis, M. tuberculosis, as well as on VERO cells for the most active compound.