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. Epub 2008 Jun 10.

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.

MeSH terms

  • Benzamides / chemistry*
  • Binding Sites
  • Chemistry, Pharmaceutical / methods
  • Diamines / chemistry
  • Drug Design
  • Humans
  • Inhibitory Concentration 50
  • Kinetics
  • Models, Chemical
  • Receptors, G-Protein-Coupled / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • Benzamides
  • Diamines
  • Receptors, G-Protein-Coupled
  • UTS2R protein, human