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

  • Bioorg Med Chem Lett. 2008 Jul 15;18(14):3950-4. doi: 10.1016/j.bmcl.2008.06.019.
Jian Jin  1 ,  Ming An ,  Anthony Sapienza ,  Nambi Aiyar ,  Diane Naselsky ,  Henry M Sarau ,  James J Foley ,  Kevin L Salyers ,  Steven D Knight ,  Richard M Keenan ,  Ralph A Rivero ,  Dashyant Dhanak ,  Stephen A Douglas
Affiliations
  • 1. Centers of Excellence for Drug Discovery, GlaxoSmithKline, 709 Swedeland Road, King of Prussia, PA 19406, USA. [email protected]
PMID: 18573659 DOI: 10.1016/j.bmcl.2008.06.019
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.