Potent small molecule CCR1 antagonists

John C Kath; William H Brissette; Matthew F Brown; Maryrose Conklyn; Amy P DiRico; Peter Dorff; Ronald P Gladue; Brett M Lillie; Paul D Lira; Erin N Mairs; William H Martin; Eric B McElroy; Molly A McGlynn; Timothy J Paradis; Christopher S Poss; Ingrid A Stock; Laurie A Tylaska; Deye Zheng

doi:10.1016/j.bmcl.2004.02.021

Potent small molecule CCR1 antagonists

Bioorg Med Chem Lett. 2004 May 3;14(9):2169-73. doi: 10.1016/j.bmcl.2004.02.021.

Authors

John C Kath¹, William H Brissette, Matthew F Brown, Maryrose Conklyn, Amy P DiRico, Peter Dorff, Ronald P Gladue, Brett M Lillie, Paul D Lira, Erin N Mairs, William H Martin, Eric B McElroy, Molly A McGlynn, Timothy J Paradis, Christopher S Poss, Ingrid A Stock, Laurie A Tylaska, Deye Zheng

Affiliation

¹ Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA. john_c_kath@groton.pfizer.com

PMID: 15081002
DOI: 10.1016/j.bmcl.2004.02.021

Abstract

The present manuscript details structure-activity relationship studies of lead structure 1, which led to the discovery of CCR1 antagonists >100-fold more potent than 1.

MeSH terms

Cell Line
Humans
Receptors, CCR1
Receptors, Chemokine / antagonists & inhibitors*
Structure-Activity Relationship

Substances

CCR1 protein, human
Receptors, CCR1
Receptors, Chemokine