Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 14, Issue 13, Pages 4610-4626Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2006.02.017
Keywords
pyranocoumarin; pharmacophore; Mycobacterium tuberculosis
Funding
- NIAID NIH HHS [1 R43 AI49053-01] Funding Source: Medline
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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 mu g/mL and respective MBC values of 32, 32, and 64 mu g/mL. (c) 2006 Elsevier Ltd. All rights reserved.
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