Design and synthesis of potent antagonists containing rigid spirocyclic privileged structures for the CGRP receptor

PV Chaturvedula, S Pin, G Tholady, CM Conway…

文献索引：Chaturvedula, Prasad V.; Pin, Sokhom; Tholady, George; Conway, Charlie M.; MacOr, John E.; Dubowchik, Gene M. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 14 p. 4719 - 4722

全文：HTML全文

被引用次数: 4

摘要

We report the synthesis of rigid spirocyclic systems as conformationally constrained variants of the Ala-Phe-NH2 dipeptide amide C-terminus of the calcitonin gene-related peptide (CGRP). CGRP receptor antagonists containing these moieties displayed potent affinity, functional antagonism and excellent oxidative stability. Structure–activity relationship studies demonstrated the relative importance of hydrogen bond donor/acceptor functionalities and ...