Structure-activity relationships for a novel series of thiazolyl phenyl ether derivatives exhibiting potent and selective acetyl-CoA carboxylase 2 inhibitory activity

Bioorg Med Chem Lett. 2006 Dec 1;16(23):6078-81. doi: 10.1016/j.bmcl.2006.08.100. Epub 2006 Sep 14.

Abstract

Structure-activity relationships for a recently discovered thiazolyl phenyl ether series of acetyl-CoA carboxylase (ACC) inhibitors were investigated. Preliminary efforts to optimize the series through modification of the distal aryl ether moiety of the lead scaffold resulted in the identification of compounds exhibiting low-nanomolar potency and isozyme-selective ACC2 activity.

MeSH terms

  • Acetyl-CoA Carboxylase / antagonists & inhibitors*
  • Acetyl-CoA Carboxylase / metabolism
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Molecular Structure
  • Phenyl Ethers / chemical synthesis
  • Phenyl Ethers / chemistry*
  • Phenyl Ethers / pharmacology*
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Phenyl Ethers
  • phenyl ether
  • Acetyl-CoA Carboxylase