Synthesis and protective effect of 1,3,5-triazine derivatives, leukotriene C4 antagonist, on HCl.ethanol-induced gastric lesions in rats.
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.
Hasegawa
Y
Y
Research Institute for Biology & Chemistry, Tsumura Co., Ltd., Ibaraki, Japan.
Yanagisawa
T
T
Okui
Y
Y
Sato
T
T
Hosaka
K
K
Chin
M S
MS
Mitsuhashi
H
H
D000818:Animals; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000431:Ethanol; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013189:SRS-A / Q000037:antagonists & inhibitors*; D013276:Stomach Ulcer / Q000139:chemically induced / Q000517:prevention & control*; D014227:Triazines / Q000138:chemical synthesis* / Q000494:pharmacology
D000897:Anti-Ulcer Agents; D013189:SRS-A; D014227:Triazines; D000431:Ethanol