Design, synthesis, and structure-activity relationship of novel CCR2 antagonists

  • Bioorg Med Chem Lett. 2009 Mar 15;19(6):1830-4. doi: 10.1016/j.bmcl.2008.12.050.
Shankaran Kothandaraman  1 ,  Karla L Donnely ,  Gabor Butora ,  Richard Jiao ,  Alexander Pasternak ,  Gregori J Morriello ,  Stephen D Goble ,  Changyou Zhou ,  Sander G Mills ,  Malcolm Maccoss ,  Pasquale P Vicario ,  Julia M Ayala ,  Julie A Demartino ,  Mary Struthers ,  Margaret A Cascieri ,  Lihu Yang
Affiliations
  • 1. Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
PMID: 19237282 DOI: 10.1016/j.bmcl.2008.12.050
Abstract

A series of novel 1-aminocyclopentyl-3-carboxyamides incorporating substituted tetrahydropyran moieties have been synthesized and subsequently evaluated for their antagonistic activity against the human CCR2 receptor. Among them analog 59 was found to posses potent antagonistic activity.