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

Shankaran Kothandaraman; 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

doi:10.1016/j.bmcl.2008.12.050

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. Epub 2008 Dec 24.

Authors

Shankaran Kothandaraman¹, 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

Affiliation

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.

MeSH terms

Administration, Oral
Animals
Chemistry, Pharmaceutical / methods*
Chemotaxis
Dogs
Drug Design
Humans
Inhibitory Concentration 50
Macaca mulatta
Models, Chemical
Molecular Structure
Rats
Rats, Sprague-Dawley
Receptors, CCR2 / antagonists & inhibitors*
Receptors, CCR2 / chemistry*
Structure-Activity Relationship

Substances

Receptors, CCR2