N-Phenyl-2-pyridinecarbothioamides as gastric mucosal protectants

Authors:
  • NLNancy E. Lee
    Nancy E. Lee
  • RBRobert M. Blank
    Robert M. Blank
  • CDChristopher A. Demerson
    Christopher A. Demerson
  • CSCarol S. Sarnella
    Carol S. Sarnella
  • NSNoreen T. Scherer
    Noreen T. Scherer
  • GMG. Nabi Mir
    G. Nabi Mir
  • LBLuis E. Borella
    Luis E. Borella
  • JDJohn F. DiJoseph
    John F. DiJoseph
  • CWCheryl Wells
    Cheryl Wells
Publisher website
Google Scholar
Abstract
A series of substituted 2-pyridinecarbothioamides was synthesized and evaluated for gastric mucosal protectant activity in the rat. Out of this investigation N-(3,5-difluorophenyl)-2- pyridinecarbothioamide (23, AY-31,574) was identified. This compound was much more potent than sucralfate and ranitidine against ethanol-induced lesions. Compound 23 was equipotent with ranitidine against gastric injury caused by stress. Unlike ranitidine, 23 was found to be devoid of antisecretory activity in the pylorus-ligated rat model, making it a selective mucosal protectant. Such a potent selective mucosal protectant may provide a novel clinical approach in treating ulcers.

This publication has 1 reference indexed in Scilit: