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

X Beebe, D Darczak, RA Davis-Taber, ME Uchic…

Index: Beebe, Xenia; Darczak, Daria; Davis-Taber, Rachel A.; Uchic, Marie E.; Scott, Victoria E.; Jarvis, Michael F.; Stewart, Andrew O. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 6 p. 2162 - 2166

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Citation Number: 19

Abstract

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. ... 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 ...