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ID: ALA1155072

Journal: Bioorg Med Chem Lett

Title: Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides.

Authors: Jin J, An M, Sapienza A, Aiyar N, Naselsky D, Sarau HM, Foley JJ, Salyers KL, Knight SD, Keenan RM, Rivero RA, Dhanak D, Douglas SA.

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 K(i) of 4 nM. The synthesis and structure-activity relationships (SAR) of N-cyclic azaalkyl benzamides are described.

CiteXplore: 18573659

DOI: 10.1016/j.bmcl.2008.06.019