Discovery of CP-533536 : An EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation

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 fr...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-04, Vol.19 (7), p.2075-2078
Hauptverfasser:	CAMERON, Kimberly O, LEFKER, Bruce A, LI YU, THOMPSON, David D, KE, Hua Z, MEI LI, ZAWISTOSKI, Michael P, TJOA, Christina M, WRIGHT, Ann S, DENINNO, Shari L, PARALKAR, Vishwas M, OWEN, Thomas A
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Male Medical sciences Osteogenesis - drug effects Pharmacology. Drug treatments Pyridines - administration & dosage Pyridines - chemistry Pyridines - pharmacokinetics Rats Rats, Sprague-Dawley Receptors, Prostaglandin E - agonists Receptors, Prostaglandin E - metabolism Receptors, Prostaglandin E, EP2 Subtype Structure-Activity Relationship Sulfonamides - chemical synthesis Sulfonamides - chemistry Sulfonamides - pharmacology
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2009.01.059