title: Synthesis and antimycobacterial evaluation of benzofurobenzopyran analogues.
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.
authors.affiliation: Laboratoire de Chimie Organique, URA 2128 CNRS-Institut Pasteur, 28 rue du Dr. Roux, 75724 Paris Cedex 15, France.
authors.forename: Soizic
authors.initials: S
authors.lastname: Prado
authors.forename: Yves L
authors.initials: YL
authors.lastname: Janin
authors.forename: Brigitte
authors.initials: B
authors.lastname: Saint-Joanis
authors.forename: Priscille
authors.initials: P
authors.lastname: Brodin
authors.forename: Sylvie
authors.initials: S
authors.lastname: Michel
authors.forename: Michel
authors.initials: M
authors.lastname: Koch
authors.forename: Stewart T
authors.initials: ST
authors.lastname: Cole
authors.forename: François
authors.initials: F
authors.lastname: Tillequin
authors.forename: Pierre-Etienne
authors.initials: PE
authors.lastname: Bost
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D002853:Chromatography, Liquid; D004353:Drug Evaluation, Preclinical; D013058:Mass Spectrometry; D051379:Mice; D008826:Microbial Sensitivity Tests; D009161:Mycobacterium / Q000187:drug effects*; D014709:Vero Cells
chemical_list: D000900:Anti-Bacterial Agents