Discovery and SAR of hydrazide antagonists of the pituitary adenylate cyclase-activating polypeptide (PACAP) receptor type 1 (PAC₁-R)

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• 作者：Xenia Beebe ; Daria Darczak ; Rachel A. Davis-Taber ; Marie E. Uchic ; Victoria E. Scott ; Michael F. Jarvis ; Andrew O. Stewart
• 关键词：PACAP ; Class B GPCR ; PAC₁-R ; Hydrazides
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2008
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 March 2008
• 卷：18
• 期：6
• 页码：2162-2166
• 文件大小：149 K

摘要

Potent small molecule antagonists for the PAC₁-R have been discovered. Previously known antagonists for the PAC₁-R were slightly truncated peptide ligands. The hydrazides reported here are the first small molecule antagonists ever reported for this class B GPCR.