Inhibitors of an essential mycobacterial cell wall lipase (Rv3802c) as tuberculosis drug leads

Chem Commun (Camb). 2011 May 14;47(18):5166-8. doi: 10.1039/c0cc05635a. Epub 2011 Mar 7.

Abstract

The first targeted inhibitors of an essential M. tuberculosis cell wall lipase, Rv3802c, are described. Lead compounds exhibited nanomolar inhibition of the enzyme, and encouraging antibacterial activity against M. tuberculosis in vitro, supporting Rv3802c as a novel TB drug target.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / antagonists & inhibitors*
  • Anti-Bacterial Agents / pharmacology*
  • Antitubercular Agents / antagonists & inhibitors*
  • Antitubercular Agents / pharmacology*
  • Bacterial Proteins / antagonists & inhibitors*
  • Cell Wall / drug effects*
  • Drug Design
  • Humans
  • Lipase / antagonists & inhibitors*
  • Mycobacterium / drug effects*
  • Mycobacterium tuberculosis / drug effects*
  • Mycobacterium tuberculosis / enzymology
  • Tuberculosis / microbiology*

Substances

  • Anti-Bacterial Agents
  • Antitubercular Agents
  • Bacterial Proteins
  • Lipase