Urotensin-II receptor antagonists: Synthesis and SAR of N-cyclic azaalkyl benzamides

J Jin, M An, A Sapienza, N Aiyar, D Naselsky…

Index: Jin, Jian; An, Ming; Sapienza, Anthony; Aiyar, Nambi; Naselsky, Diane; Sarau, Henry M.; Foley, James J.; Salyers, Kevin L.; Knight, Steven D.; Keenan, Richard M.; Rivero, Ralph A.; Dhanak, Dashyant; Douglas, Stephen A. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 14 p. 3950 - 3954

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Citation Number: 12

Abstract

SAR exploration of the central diamine, benzyl, and terminal aminoalkoxy regions of the N- cyclic azaalkyl benzamide series led to the identification of very potent human urotensin-II receptor antagonists such as 1a with a Ki of 4nM. The synthesis and structure–activity relationships (SAR) of N-cyclic azaalkyl benzamides are described.