The synthesis and vasopressin (AVP) antagonist activity of a novel series of N-aroyl-2,4,5,6-tetrahydropyrazolo[3,4-d]thieno[3,2-b]azepines

Bioorg Med Chem Lett. 2000 Apr 17;10(8):695-8. doi: 10.1016/s0960-894x(00)00084-6.

Abstract

Synthesis and SAR of N-[4-[(4,5-dihydropyrazolo[3,4-d]thieno[3,2-b]azepin-6(2H)-y l)carbonyl]phenyl]benzamides as arginine vasopressin (AVP) receptor antagonists are discussed. Potent orally active AVP receptor antagonists are produced when the benzamide moiety contains a phenyl group at the 2-position. Similar analogues of 4,6,7,8-tetrahydro-5H-thieno[3,2-b]azepine and VPA-985 are reported.

MeSH terms

  • Animals
  • Arginine Vasopressin / antagonists & inhibitors*
  • Arginine Vasopressin / metabolism
  • Azepines / chemical synthesis*
  • Azepines / chemistry
  • Azepines / metabolism
  • Azepines / pharmacology*
  • Rats
  • Receptors, Vasopressin / metabolism
  • Structure-Activity Relationship

Substances

  • Azepines
  • Receptors, Vasopressin
  • Arginine Vasopressin