title: Optimization of CCR4 antagonists: side-chain exploration.
abstract: The design, synthesis, and activity of novel and selective small molecule antagonists of the CC chemokine receptor-4 (CCR4) are presented. Compound 8c was efficacious in a murine allergic inflammation model (ED(50) 30 mg/kg).
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA. ashok.purandare@bms.com
authors.forename: Ashok V
authors.initials: AV
authors.lastname: Purandare
authors.forename: Honghe
authors.initials: H
authors.lastname: Wan
authors.forename: Aiming
authors.initials: A
authors.lastname: Gao
authors.forename: John
authors.initials: J
authors.lastname: Somerville
authors.forename: Christine
authors.initials: C
authors.lastname: Burke
authors.forename: Wayne
authors.initials: W
authors.lastname: Vaccaro
authors.forename: Xiaoxia
authors.initials: X
authors.lastname: Yang
authors.forename: Kim W
authors.initials: KW
authors.lastname: McIntyre
authors.forename: Michael A
authors.initials: MA
authors.lastname: Poss
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D018925:Chemokines / Q000378:metabolism; D002633:Chemotaxis; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D004804:Eosinophils / Q000378:metabolism; D006967:Hypersensitivity; D007249:Inflammation; D020128:Inhibitory Concentration 50; D007962:Leukocytes / Q000166:cytology; D051379:Mice; D008956:Models, Chemical; D054398:Receptors, CCR4; D019707:Receptors, Chemokine / Q000037:antagonists & inhibitors*; D015398:Signal Transduction; D013329:Structure-Activity Relationship
chemical_list: C515355:Ccr4 protein, mouse; D018925:Chemokines; D054398:Receptors, CCR4; D019707:Receptors, Chemokine