Pyranocoumarin, a novel anti-TB pharmacophore: synthesis and biological evaluation against Mycobacterium tuberculosis.
Pyranocoumarin compounds were identified to embody a novel and unique pharmacophore for anti-TB activity. A systematic approach was taken to investigate the structural characteristics. Focused libraries of compounds were synthesized and evaluated for their anti-TB activity in primary screening assays. Compounds shown to be active were further determined for MIC and MBC values. Three of the four bactericidal compounds (16, 17c, and 18f) were amino derivatives, with MIC values of 16 microg/mL and respective MBC values of 32, 32, and 64 microg/mL.
Xu
Ze-Qi
ZQ
Advanced Life Sciences, Inc., Woodridge, IL 60517, USA. zxu@advancedlifesciences.com
Pupek
Krzysztof
K
Suling
William J
WJ
Enache
Livia
L
Flavin
Michael T
MT
D000904:Antibiotics, Antitubercular / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D039681:Pyranocoumarins / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
D000904:Antibiotics, Antitubercular; D039681:Pyranocoumarins