Coordination chemistry based approach to lipophilic inhibitors of 1-deoxy-D-xylulose-5-phosphate reductoisomerase

Lisheng Deng, Sandeep Sundriyal, Valentina Rubio Calva, Zheng-Zheng Shi, Yongcheng Song

Research output: Contribution to journalArticle

49 Scopus citations

Abstract

1-Deoxy-D-xylulose-5-phosphate reductoisomerase (DXR) in the non-mevalonate pathway found in most bacteria is a validated anti-infective drug target. Fosmidomycin, a potent DXR inhibitor, is active against Gram-negative bacteria. A coordination chemistry and structure based approach was used to discover a novel, lipophilic DXR inhibitor with an IC50 of 1.4 μM. It exhibited a broad spectrum of activity against Gram-negative and -positive bacteria with minimal inhibition concentrations of 20-100 μM (or 3.7-19 μg/mL).

Original languageEnglish (US)
Pages (from-to)6539-6542
Number of pages4
JournalJournal of Medicinal Chemistry
Volume52
Issue number21
DOIs
StatePublished - Nov 12 2009

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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