Antidotes to anthrax lethal factor intoxication. Part 1: Discovery of potent lethal factor inhibitors with in vivo efficacy

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6850-3. doi: 10.1016/j.bmcl.2010.08.058. Epub 2010 Aug 15.

Abstract

Sub-nanomolar small molecule inhibitors of anthrax lethal factor have been identified using SAR and Merck L915 (4) as a model compound. One of these compounds (16) provided 100% protection in a rat lethal toxin model of anthrax disease.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, N.I.H., Intramural

MeSH terms

  • Animals
  • Antidotes / chemistry
  • Antidotes / pharmacology*
  • Antigens, Bacterial
  • Bacterial Toxins / antagonists & inhibitors*
  • Rats
  • Structure-Activity Relationship

Substances

  • Antidotes
  • Antigens, Bacterial
  • Bacterial Toxins
  • anthrax toxin