(4-Substituted-phenyl)-(5H-10,11-dihydro-pyrrolo [2,1-c][1,4] benzodiazepin-10-yl)-methanone derivatives as vasopressin receptor modulators

Bioorg Med Chem Lett. 2005 Nov 15;15(22):5003-6. doi: 10.1016/j.bmcl.2005.08.007.

Abstract

Synthesis and structure-activity relationships (SAR) of arginine vasopressin (AVP) receptor modulators are described. Potent and selective compounds are prepared when the amide linkage connecting rings A and B of VPA-985 is replaced with a bond, CO, -O-, -S-, or -SO2- bond.

MeSH terms

  • Antidiuretic Hormone Receptor Antagonists
  • Benzodiazepines / chemical synthesis*
  • Benzodiazepines / chemistry
  • Benzodiazepines / pharmacology*
  • Blood Platelets / drug effects
  • Blood Platelets / metabolism
  • Humans
  • Inhibitory Concentration 50
  • Molecular Structure
  • Pyrroles / chemical synthesis*
  • Pyrroles / chemistry
  • Pyrroles / pharmacology*
  • Receptors, Vasopressin / metabolism*
  • Sensitivity and Specificity
  • Structure-Activity Relationship

Substances

  • Antidiuretic Hormone Receptor Antagonists
  • Pyrroles
  • Receptors, Vasopressin
  • Benzodiazepines