Second-generation dimeric inhibitors of chitin synthase

Bioorg Med Chem. 2004 Dec 15;12(24):6451-60. doi: 10.1016/j.bmc.2004.09.027.

Abstract

Chitin synthase (CS) is essential for fungal cell wall biosynthesis and is an attractive medicinal target. Expanded results from our efforts to develop mechanism based inhibitors of CS are presented here. Specifically, we describe uridine dimers linked by tartrate amides as potential pyrophosphate mimics.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Antifungal Agents / chemical synthesis*
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology
  • Chitin Synthase / antagonists & inhibitors*
  • Cross-Linking Reagents
  • Dimerization
  • Enzyme Inhibitors / chemistry
  • Structure-Activity Relationship
  • Tartrates
  • Uridine

Substances

  • Antifungal Agents
  • Cross-Linking Reagents
  • Enzyme Inhibitors
  • Tartrates
  • Chitin Synthase
  • tartaric acid
  • Uridine