Sato Y, Shimoji Y, Fujita H, Nishino H, Mizuno H, Kobayashi S, Kumakura S
J Med Chem. 1980 Aug;23(8):927-37. doi: 10.1021/jm00182a021.
The synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to pyrrole, thiophene, pyran, pyridine, and pyridazine are described. Among these compounds, 8-tert-butyl-7,8-dihydro-5-methyl-6H-pyrrolo[3,2-e][1,2,4]triazolo[1,5-a]pyrimidine (23) was found to be the most promising potential cardiovascular agent, having been shown to be more potent in coronary vasodilating activity than trapidil [7-diethylamino)-5-methyl-1,2,4-triazolo[1,5-a]pyrimidine] and approximately equipotent to guanethidine sulfate in antihypertensive activity.
描述了与吡咯、噻吩、吡喃、吡啶和哒嗪稠合的1,2,4-三唑并[1,5-a]嘧啶的合成及其冠状血管舒张和抗高血压活性。在这些化合物中，8-叔丁基-7,8-二氢-5-甲基-6H-吡咯并[3,2-e][1,2,4]三唑并[1,5-a]嘧啶（23）被发现是最有前景的潜在心血管药物，已证明其冠状血管舒张活性比曲匹地尔[7-二乙氨基)-5-甲基-1,2,4-三唑并[1,5-a]嘧啶]更强，且抗高血压活性与硫酸胍乙啶大致相当。
