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

被引：25

作者：

Cameron, Kimberly O. ^{[1
]}

Lefker, Bruce A. ^{[1
]}

Ke, Hua Z. ^{[2
]}

Li, Mei ^{[1
]}

Zawistoski, Michael P. ^{[1
]}

Tjoa, Christina M. ^{[1
]}

Wright, Ann S. ^{[1
]}

DeNinno, Shari L. ^{[1
]}

Paralkar, Vishwas M. ^{[1
]}

Owen, Thomas A. ^{[3
]}

Yu, Li ^{[4
]}

Thompson, David D. ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Groton Labs, Dept Cardiovasc & Metab Dis, Groton, CT 06340 USA

[2] Amgen Inc, Thousand Oaks, CA 91320 USA

[3] Ramapo Coll, Dept Theoret & Appl Sci, Mahwah, NJ 07430 USA

[4] Millennium Pharmaceut Inc, Cambridge, MA 02139 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 07期

关键词：

Prostaglandin; EP2; receptor; Fracture healing; Bone; MASS; RATS;

D O I：

10.1016/j.bmcl.2009.01.059

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：2075 / 2078

页数：4

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