title: Novel pyrrolidine heterocycles as CCR1 antagonists.
abstract: A novel series of pyrrolidine heterocycles was prepared and found to show potent inhibitory activity of CCR1 binding and CCL3 mediated chemotaxis of a CCR1-expressing cell line. A potent, optimized triazole lead from this series was found to have acceptable pharmacokinetics and microsomal stability in rat and is suitable for further optimization and development.
authors: Ligand Pharmaceuticals, Inc., 3000 Eastpark Blvd., Cranbury, NJ 08512, USA. jmerritt@kean.edu
authors: J Robert
authors: JR
authors: Merritt
authors: Ray
authors: R
authors: James
authors: Vidyadhar M
authors: VM
authors: Paradkar
authors: Chongwu
authors: C
authors: Zhang
authors: Ruiyan
authors: R
authors: Liu
authors: Jinqi
authors: J
authors: Liu
authors: Biji
authors: B
authors: Jacob
authors: Camelia
authors: C
authors: Chiriac
authors: Michael J
authors: MJ
authors: Ohlmeyer
authors: Elizabeth
authors: E
authors: Quadros
authors: Pamela
authors: P
authors: Wines
authors: Jennifer
authors: J
authors: Postelnek
authors: Catherine M
authors: CM
authors: Hicks
authors: Weiqing
authors: W
authors: Chen
authors: Earl F
authors: EF
authors: Kimble
authors: Linda
authors: L
authors: O'Brien
authors: Nicole
authors: N
authors: White
authors: Hema
authors: H
authors: Desai
authors: Kenneth C
authors: KC
authors: Appell
authors: Maria L
authors: ML
authors: Webb
mesh_terms: D000818:Animals; D002460:Cell Line; D054405:Chemokine CCL3 / Q000276:immunology*; D002633:Chemotaxis / Q000187:drug effects*; D008862:Microsomes, Liver / Q000378:metabolism; D011759:Pyrrolidines / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D054389:Receptors, CCR1 / Q000037:antagonists & inhibitors* / Q000276:immunology; D014230:Triazoles / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D054405:Chemokine CCL3; D011759:Pyrrolidines; D054389:Receptors, CCR1; D014230:Triazoles; C032519:pyrrolidine