N-Substituted pyrazole-3-carboxamides as inhibitors of human 15-lipoxygenase

Bioorg Med Chem Lett. 2015 Aug 1;25(15):3017-23. doi: 10.1016/j.bmcl.2015.05.007. Epub 2015 May 15.

Abstract

High-throughput screening was used to find selective inhibitors of human 15-lipoxygenase-1 (15-LOX-1). One hit, a 1-benzoyl substituted pyrazole-3-carboxanilide (1a), was used as a starting point in a program to develop potent and selective 15-LOX-1 inhibitors.

Keywords: 15-Lipoxygenase; Arachidonic acid; Inhibitors; Pyrazole.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemistry
  • Amides / pharmacology
  • Arachidonate 15-Lipoxygenase / metabolism*
  • Humans
  • Lipoxygenase Inhibitors / chemistry*
  • Lipoxygenase Inhibitors / pharmacology*
  • Pyrazoles / chemistry*
  • Pyrazoles / pharmacology*

Substances

  • Amides
  • Lipoxygenase Inhibitors
  • Pyrazoles
  • pyrazole
  • Arachidonate 15-Lipoxygenase