2. Academic Validation
  3. Structure-activity relationships of compounds targeting mycobacterium tuberculosis 1-deoxy-D-xylulose 5-phosphate synthase

Structure-activity relationships of compounds targeting mycobacterium tuberculosis 1-deoxy-D-xylulose 5-phosphate synthase

  • Bioorg Med Chem Lett. 2008 Oct 1;18(19):5320-3. doi: 10.1016/j.bmcl.2008.08.034.
Jialin Mao 1,  Hyungjin Eoh,  Rong He,  Yuehong Wang,  Baojie Wan,  Scott G Franzblau,  Dean C Crick,  Alan P Kozikowski
Affiliations

Affiliation

  • 1 Drug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL 60612, USA.
PMID: 18783951 DOI: 10.1016/j.bmcl.2008.08.034
Abstract

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-benzyl-4H-pyrazolo[1,5-a]pyrimidin-7-one. Ultimately we found that 2-methyl-3-(4-fluorophenyl)-5-(4-methoxy-phenyl)-4H-pyrazolo[1,5-a]pyrimidin-7-one, although still weak, was able to inhibit M. tuberculosis DXS with an IC(50) of 10.6 microM.

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