(E)-Phenyl- and -heteroaryl-substituted O-benzoyl-(or acyl)oximes as lipoprotein-associated phospholipase A2 inhibitors

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1525-7. doi: 10.1016/j.bmcl.2004.11.063.

Abstract

A series of (E)-phenyl- and -heteroaryl-substituted O-benzoyl- (or acyl)oximes 3a-n were synthesized for evaluating their human lipoprotein-associated phospholiphase A2 (Lp-PLA2) inhibitory activities. The less lipophilic derivatives 3a-c showed the most potent in vitro inhibitory activity on human Lp-PLA2.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 1-Alkyl-2-acetylglycerophosphocholine Esterase
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Molecular Structure
  • Oximes / chemical synthesis
  • Oximes / chemistry
  • Oximes / pharmacology*
  • Phospholipases A / antagonists & inhibitors*
  • Phospholipases A2
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Oximes
  • Phospholipases A
  • Phospholipases A2
  • 1-Alkyl-2-acetylglycerophosphocholine Esterase