[Studies on the synthesis of cholecystokinin A receptor antagonists. II. Synthesis and cholecystokinin A receptor inhibitory activities of sulfur-containing amide-carboxylic acid derivatives]

Yakugaku Zasshi. 1996 May;116(5):396-410. doi: 10.1248/yakushi1947.116.5_396.
[Article in Japanese]

Abstract

A number of sulfur-containing amide-carboxylic acid derivatives were synthesized and tested for cholecystokinin A (CCK-A) receptor inhibitory activity in order to study structure-activity relationships. Significant CCK-A receptor inhibitory activities were found in only two series, that is, sulfoxide-carboxylic acid derivatives (9) and sulfone-carboxylic acid derivatives (10). As the most preferred compound, 5-(3,4-dichlorophenylsulfonyl)-4-(N,N-dipentylcarbamoyl)pent anoic acid (10n) was selected.

Publication types

  • English Abstract

MeSH terms

  • Animals
  • In Vitro Techniques
  • Male
  • Rats
  • Rats, Wistar
  • Receptor, Cholecystokinin A
  • Receptors, Cholecystokinin / antagonists & inhibitors*
  • Structure-Activity Relationship
  • Sulfides / pharmacology*
  • Sulfones / pharmacology*
  • Sulfoxides / pharmacology*

Substances

  • Receptor, Cholecystokinin A
  • Receptors, Cholecystokinin
  • Sulfides
  • Sulfones
  • Sulfoxides