带有利多氟嗪药效基团片段的1,4 - 二氢吡啶类化合物。
1,4-Dihydropyridines bearing a pharmacophoric fragment of lidoflazine.
作者信息
Chiarini A, Rampa A, Budriesi R, Bisi A, Fabbri G, Valenti P
机构信息
Department of Pharmaceutical Sciences, University of Bologna, Italy.
出版信息
Bioorg Med Chem. 1996 Oct;4(10):1629-35. doi: 10.1016/0968-0896(96)00155-1.
A series of 1,4-dihydropyridines bearing a pharmacophoric fragment of lidoflazine was synthesized. The compounds were evaluated for inotropic, chronotropic, and calcium antagonist activities. All compounds behave as inotropic and chronotropic agents, except for compounds 4b, 5a, and 5b, which exhibit a rather weak calcium antagonism in vascular smooth muscle (like aorta). Compound 5b is about twofold more potent in decreasing both chronotropy and inotropy, while compound 5c is about fivefold more potent in decreasing inotropy than nifedipine. Moreover, compound 5b is the most potent calcium antagonist derivative of the series.
合成了一系列带有利多氟嗪药效团片段的1,4 - 二氢吡啶。对这些化合物进行了变力性、变时性和钙拮抗剂活性评估。除化合物4b、5a和5b外，所有化合物均表现为变力性和变时性药物，化合物4b、5a和5b在血管平滑肌（如主动脉）中表现出相当弱的钙拮抗作用。化合物5b在降低变时性和变力性方面的效力约为其他化合物的两倍，而化合物5c在降低变力性方面的效力比硝苯地平高约五倍。此外，化合物5b是该系列中最有效的钙拮抗剂衍生物。
Zotero 插件