Synthesis and protective effect of 1,3,5-triazine derivatives, leukotriene C4 antagonist, on HCl.ethanol-induced gastric lesions in rats

Chem Pharm Bull (Tokyo). 1991 Dec;39(12):3180-2. doi: 10.1248/cpb.39.3180.

Abstract

2,4-Diamino-[E]-6-[2-(3-pyridyl)ethenyl]-1,3,5-triazine (3a), leukotriene C4 (LTC4) antagonist, was found to possess a protective effect on HCl.ethanol-induced gastric lesions. Analogues of 3a were synthesized and evaluated for the effect as well as antagonistic activity against LTC4-induced contraction. Seven compounds (3a-d, f-h) exhibited a potent protective effect on gastric lesions which was considered to be based on the antagonistic activity against LTC4. The structure-activity relationships of the derivatives (3a-k) are discussed.

MeSH terms

  • Animals
  • Anti-Ulcer Agents / chemical synthesis*
  • Anti-Ulcer Agents / pharmacology
  • Ethanol*
  • Guinea Pigs
  • In Vitro Techniques
  • Male
  • Rats
  • Rats, Inbred Strains
  • SRS-A / antagonists & inhibitors*
  • Stomach Ulcer / chemically induced
  • Stomach Ulcer / prevention & control*
  • Triazines / chemical synthesis*
  • Triazines / pharmacology

Substances

  • Anti-Ulcer Agents
  • SRS-A
  • Triazines
  • Ethanol