Synthesis and antimycobacterial evaluation of benzofurobenzopyran analogues.
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.
Prado
Soizic
S
Laboratoire de Chimie Organique, URA 2128 CNRS-Institut Pasteur, 28 rue du Dr. Roux, 75724 Paris Cedex 15, France.
Janin
Yves L
YL
Saint-Joanis
Brigitte
B
Brodin
Priscille
P
Michel
Sylvie
S
Koch
Michel
M
Cole
Stewart T
ST
Tillequin
François
F
Bost
Pierre-Etienne
PE
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
D000900:Anti-Bacterial Agents