Discovery of a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists

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• 作者：Masaki Asada ; Tetsuo Obitsu ; Toshihiko Nagase ; Isamu Sugimoto ; Yoshiyuki Yamaura ; Kazutoyo Sato ; Masami Narita ; Shuichi Ohuchida ; Hisao Nakai ; Masaaki Toda
• 关键词：Prostaglandin ; EP3 receptor ; Antagonist ; Pyrazole
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2009
• 出版时间：15 September 2009
• 年：2009
• 卷：17
• 期：18
• 页码：6567-6582
• 全文大小：1500 K

文摘

A series of acrylic acids and their structurally related compounds were evaluated for their binding affinity to four EP receptor subtypes (EP1-4). Starting from the initial hit 3, which was discovered in our in-house library, compounds 4 and 5 were identified as new chemical leads as candidates for further optimization towards a selective EP3 receptor antagonist. The identification process of these compounds and their pharmacokinetic profiles are presented.