Design, synthesis, and in vitro activity of bis (succinimido) hexane peptide heterodimers with combined B1 and B2 antagonist activity

JC Cheronis, ET Whalley, LG Allen…

Index: Cheronis, John C.; Whalley, Eric T.; Allen, Lisa G.; Loy, Sharon D.; Elder, Megan W.; et al. Journal of Medicinal Chemistry, 1994 , vol. 37, # 3 p. 348 - 355

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Citation Number: 29

Abstract

We have developed a series of peptide heterodimers based on the B2 antagonist~-Are- [Hyp~,~-Phe7, Leu8]-BK (1) and the B1 antagonist LysO-[Leus, des-Arg91-BK (7) that are potent antagonists of both B1 and B2 receptors. From this series, compound 50 (alternatively, CP-0364), the 1, 6-bis (succinimido) hexane heterodimer of~-ArgO-[Hyp~, Cys~,~-Phe~, Leu~ l-BK (2), and D-ArgO-[Cysl,-Hyp3, Leu8, des-Argg]-BK (6), was found ...