Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 19, Pages 5320-5323Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.08.034
Keywords
drug design; DXS; enzyme; SAR; tuberculosis
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Funding
- NIAID NIH HHS [R01 AI097550] Funding Source: Medline
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We report on a target- based approach to identify possible Mycobacterium tuberculosis DXS inhibitors from the structure of a known transketolase inhibitor. A small focused library of analogs was assembled in order to begin elucidating some meaningful structure - activity relationships of 3-(4-chloro-phenyl)-5-benzyl4H-pyrazolo[ 1,5-a]pyrimidin-7-one. Ultimately we found that 2-methyl-3-(4-fluorophenyl)-5-(4-methoxyphenyl)-4H-pyrazolo[1,5-a]pyrimidin-7-one, although still weak, was able to inhibit M. tuberculosis DXS with an IC50 of 10.6 mu M. (c) 2008 Elsevier Ltd. All rights reserved.
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