title: The discovery of structurally novel CCR1 antagonists derived from a hydroxyethylene peptide isostere template.
abstract: The present manuscript details the discovery and early fundamental structure-activity relationship studies involving compound 3, a novel hydroxyethylene peptide isostere derived molecule that provides micromolar inhibition of CCL3 binding to its receptor CCR1. Initial studies established this screening hit as a legitimate lead for further medicinal chemistry optimization.
authors.affiliation: Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA. john_c_kath@groton.pfizer.com
authors.forename: John C
authors.initials: JC
authors.lastname: Kath
authors.forename: Amy P
authors.initials: AP
authors.lastname: DiRico
authors.forename: Ronald P
authors.initials: RP
authors.lastname: Gladue
authors.forename: William H
authors.initials: WH
authors.lastname: Martin
authors.forename: Eric B
authors.initials: EB
authors.lastname: McElroy
authors.forename: Ingrid A
authors.initials: IA
authors.lastname: Stock
authors.forename: Laurie A
authors.initials: LA
authors.lastname: Tylaska
authors.forename: Deye
authors.initials: D
authors.lastname: Zheng
mesh_terms: D018360:Crystallography, X-Ray; D010455:Peptides / Q000737:chemistry / Q000494:pharmacology*; D011487:Protein Conformation; D054389:Receptors, CCR1; D019707:Receptors, Chemokine / Q000037:antagonists & inhibitors*
chemical_list: D010455:Peptides; D054389:Receptors, CCR1; D019707:Receptors, Chemokine