Antimycobacterial evaluation of germacranolides.
The minimum inhibitory concentrations (MIC) against Mycobacterium tuberculosis and M. avium of parthenolide, costunolide, 1 (10)-epoxycostunolide and other germacranolide-type sesquiterpene lactones and derivatives were determined by use of a radiorespirometric bioassay. Structure-activity relationship studies with natural and semisynthetic sesquiterpene lactones suggested that the alpha-methylene-gamma-lactone moiety is an essential, but not sufficient, structural requirement for significant in vitro activity against M. tuberculosis and M. avium.
Fischer
N H
NH
Department of Chemistry, Louisiana State University, Baton Rouge 70803-1804, USA. fischer@chemgate.chem.lsu.edu
Lu
T
T
Cantrell
C L
CL
Castañeda-Acosta
J
J
Quijano
L
L
Franzblau
S G
SG
D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D009162:Mycobacterium avium / Q000187:drug effects*; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D012717:Sesquiterpenes / Q000494:pharmacology*; D007783:Lactones
D000900:Anti-Bacterial Agents; D012717:Sesquiterpenes; C002669:parthenolide; C002602:costunolide; D007783:Lactones