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

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• 作者：Kimberly O. Cameron ; Bruce A. Lefker ; Hua Z. Ke ; Mei Li ; Michael P. Zawistoski ; Christina M. Tjoa ; Ann S. Wright ; Shari L. DeNinno ; Vishwas M. Paralkar ; Thomas A. Owen ; Li Yu ; David D. Thompson
• 关键词：Prostaglandin ; EP₂ receptor ; Fracture healing ; Bone
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 出版时间：1 April 2009
• 年：2009
• 卷：19
• 期：7
• 页码：2075-2078
• 全文大小：605 K

文摘

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.