4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 7, Pages 2075-2078

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.01.059

Keywords

Prostaglandin; EP2 receptor; Fracture healing; Bone

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Sulfonamides, exemplified by 3a, were identified as highly selective EP2 agonists. Lead optimization led to the identification of CP-533536, 7f, a potent and selective EP2 agonist. CP-533536 demonstrated the ability to heal fractures when administered locally as a single dose in rat models of fracture healing. (C) 2009 Elsevier Ltd. All rights reserved.

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