2. Academic Validation
  3. Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides

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

Affiliation

  • 1 Centers of Excellence for Drug Discovery, GlaxoSmithKline, 709 Swedeland Road, King of Prussia, PA 19406, USA. jian.jin@gsk.com
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.

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