Discovery of diarylacrylonitriles as a novel series of small molecule sortase A inhibitors

J Med Chem. 2004 May 6;47(10):2418-21. doi: 10.1021/jm0498708.

Abstract

On the basis of a hit from random screening, a novel class of small-molecule sortase A inhibitors was generated. The primary structure-activity relationship and the minimal structural requirements for potency were established through structural modifications and molecular modeling studies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylonitrile / analogs & derivatives*
  • Acrylonitrile / chemical synthesis*
  • Acrylonitrile / chemistry
  • Aminoacyltransferases / antagonists & inhibitors*
  • Bacterial Proteins
  • Cysteine Endopeptidases
  • Kinetics
  • Models, Molecular
  • Structure-Activity Relationship

Substances

  • Bacterial Proteins
  • Aminoacyltransferases
  • sortase A
  • Cysteine Endopeptidases
  • Acrylonitrile