Synthesis and Antihistaminic Activity of Some thiazolidin-4-ones

J Med Chem. 1992 Jul 24;35(15):2910-2. doi: 10.1021/jm00093a025.

Abstract

A new series of 2-(4- and 3-substituted phenyl)-3-[3-(N,N-dimethylamino) propyl]-1,3-thiazolidin-4-ones were synthesized, characterized, and evaluated for their ability to inhibit the contractions induced by histamine on guinea pig ileum. The measurement of pA2 values suggested that the reported compounds showed H1-antagonism. The more active compounds 5, 9, and 13 exhibited activity close to that of mepyramine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Female
  • Guinea Pigs
  • Histamine H1 Antagonists / chemical synthesis*
  • Histamine H1 Antagonists / pharmacology
  • Ileum / drug effects
  • In Vitro Techniques
  • Magnetic Resonance Spectroscopy
  • Male
  • Structure-Activity Relationship
  • Thiazoles / chemical synthesis*
  • Thiazoles / pharmacology
  • X-Ray Diffraction

Substances

  • Histamine H1 Antagonists
  • Thiazoles