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Studies on cardiovascular agents. 6. Synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to heterocyclic systems.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 1980-08-01 , DOI: 10.1021/jm00182a021
Yasunobu Sato , Yasuo Shimoji , Hiroshi Fujita , Hiroshi Nishino , Hiroshi Mizuno , Shinsaku Kobayashi , Seiji Kumakura

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.

中文翻译:

心血管药物的研究。6.与杂环系统融合的1,2,4-三唑并[1,5-a]嘧啶的合成及其冠状血管舒张和降压活性。

描述了与吡咯,噻吩,吡喃,吡啶和哒嗪融合的1,2,4-三唑并[1,5-a]嘧啶的合成及其冠状血管舒张和降压活性。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)为被发现是最有前途的潜在心血管疾病药物,已被证明比特拉迪尔[7-二乙基氨基)-5-甲基-1,2,4-三唑并[1,5-a]嘧啶具有更强的冠脉扩张活性,降压活性与硫酸胍乙当量相当。
更新日期:2019-11-01
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