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

被引:29
作者
Beebe, Xenia [1 ]
Darczak, Daria [1 ]
Davis-Taber, Rachel A. [1 ]
Uchic, Marie E. [1 ]
Scott, Victoria E. [1 ]
Jarvis, Michael F. [1 ]
Stewart, Andrew O. [1 ]
机构
[1] Abbott Labs, Abbott Pk, IL 60064 USA
关键词
PACAP; class B GPCR; PAC(1)-R; hydrazides;
D O I
10.1016/j.bmcl.2008.01.052
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
Potent small molecule antagonists for the PAC(1)-R have been discovered. Previously known antagonists for the PAC(1)-R were slightly truncated peptide ligands. The hydrazides reported here are the first small molecule antagonists ever reported for this class B GPCR. (C) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2162 / 2166
页数:5
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