2-Aminomethyl piperidines as novel urotensin-II receptor antagonists

J Jin, Y Wang, F Wang, D Shi, KF Erhard, Z Wu…

Index: Jin, Jian; Wang, Yonghui; Wang, Feng; Shi, Dongchuan; Erhard, Karl F.; Wu, Zining; Guida, Brian F.; Lawrence, Sarah K.; Behm, David J.; Disa, Jyoti; Vaidya, Kalindi S.; Evans, Christopher; McMillan, Lynette J.; Rivero, Ralph A.; Neeb, Michael J.; Douglas, Stephen A. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 9 p. 2860 - 2864

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Citation Number: 13

Abstract

A series of 2-aminomethyl piperidines has been discovered as novel urotensin-II receptor antagonists. The synthesis, initial structure-activity relationships, and optimization of the initial hit that resulted in the identification of potent, cross-species active, and functional urotensin-II receptor antagonists such as 1a and 11a are described.