title: Discovery of CP-533536: an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation.
abstract: Sulfonamides, exemplified by 3a, were identified as highly selective EP(2) agonists. Lead optimization led to the identification of CP-533536, 7f, a potent and selective EP(2) agonist. CP-533536 demonstrated the ability to heal fractures when administered locally as a single dose in rat models of fracture healing.
authors.affiliation: Department of Cardiovascular and Metabolic Diseases, Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA. kimberly.o.cameron@pfizer.com
authors.forename: Kimberly O
authors.initials: KO
authors.lastname: Cameron
authors.forename: Bruce A
authors.initials: BA
authors.lastname: Lefker
authors.forename: Hua Z
authors.initials: HZ
authors.lastname: Ke
authors.forename: Mei
authors.initials: M
authors.lastname: Li
authors.forename: Michael P
authors.initials: MP
authors.lastname: Zawistoski
authors.forename: Christina M
authors.initials: CM
authors.lastname: Tjoa
authors.forename: Ann S
authors.initials: AS
authors.lastname: Wright
authors.forename: Shari L
authors.initials: SL
authors.lastname: DeNinno
authors.forename: Vishwas M
authors.initials: VM
authors.lastname: Paralkar
authors.forename: Thomas A
authors.initials: TA
authors.lastname: Owen
authors.forename: Li
authors.initials: L
authors.lastname: Yu
authors.forename: David D
authors.initials: DD
authors.lastname: Thompson
mesh_terms: D000818:Animals; D008297:Male; D010012:Osteogenesis / Q000187:drug effects*; D011725:Pyridines / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D018078:Receptors, Prostaglandin E / Q000819:agonists* / Q000378:metabolism; D058307:Receptors, Prostaglandin E, EP2 Subtype; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: C475539:CP533536; C545646:Ptger2 protein, rat; D011725:Pyridines; D018078:Receptors, Prostaglandin E; D058307:Receptors, Prostaglandin E, EP2 Subtype; D013449:Sulfonamides