作为钙拮抗剂的咪唑并[1,5 - a]嘧啶和苯并[4,5]咪唑并[1,2 - a]嘧啶衍生物
Imidazo[1,5-a]pyrimidine and benzo[4,5]imidazo-[1,2-a]pyrimidine derivatives as calcium antagonists.
作者信息
Alajarin R, Vaquero J J, Alvarez-Builla J, de Casa-Juana M F, Sunkel C, Priego J G, Gomez-Sal P, Torres R
机构信息
Departamento de Química Orgánica, Universidad de Alcalá, Alcalá de Henares, Madrid, Spain.
出版信息
Bioorg Med Chem. 1994 May;2(5):323-9. doi: 10.1016/s0968-0896(00)82188-4.
Several bicyclic dihydropyrimidines were synthesized and evaluated for their calcium antagonistic activities by comparison with the usual 1,4-dihydropyridine calcium antagonist reference compound nifedipine. The solid-state structure of the isopropyl 2-methyl-4-(3'-nitrophenyl)-1,4-dihydrobenzo[4,5]imidazo[1,2- a]pyrimido-3-carboxylate shows that these compounds can adopt the most important structural features of the 1,4-dihydropyridine and 1,4-dihydropyrimidine calcium channel blockers. The high-potassium depolarized rat aorta assay was used for testing the compounds as calcium channel blockers. Some compounds showed interesting vasorelaxant activity.
合成了几种双环二氢嘧啶，并通过与常用的1,4-二氢吡啶类钙拮抗剂参考化合物硝苯地平比较，评估了它们的钙拮抗活性。2-甲基-4-(3'-硝基苯基)-1,4-二氢苯并[4,5]咪唑并[1,2-a]嘧啶-3-羧酸异丙酯的固态结构表明，这些化合物可以呈现1,4-二氢吡啶和1,4-二氢嘧啶类钙通道阻滞剂的最重要结构特征。采用高钾去极化大鼠主动脉试验来测试这些化合物作为钙通道阻滞剂的活性。一些化合物表现出有趣的血管舒张活性。
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