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  • Title: Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides.
    Author: 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.
    Journal: Bioorg Med Chem Lett; 2008 Jul 15; 18(14):3950-4. PubMed ID: 18573659.
    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.
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