Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: Synthesis and pharmacological evaluation
Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: Synthesis and pharmacological evaluation
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DOI：
10.1016/j.ejmech.2010.08.022
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发表时间：
2010-11-01
影响因子：
6.7
通讯作者：
Gilani, Sadaf J.
中科院分区：
文献类型：
--
作者：
Alam, Ozair;Khan, Suroor A.;Gilani, Sadaf J.
根据降压药效团模型的结构要求，设计合成了一系列5-（4-取代苯基）-2-（取代苄基磺酰）-4-（取代苯基）-6-甲基-1,4-二氢-5-嘧啶类羧胺（1-30）。采用大鼠无创血压（NIBP）测量法（尾袖法）检测所有合成化合物的降压活性。与对照组相比，几乎所有被测试的化合物都显示血压明显下降。13种化合物显示出与标准药物硝苯地平相当的显著降压活性。(C) 2010 Elsevier Masson SAS。版权所有。
A number of 5-(4-substituted phenyl)-2-(substiruted benzylsulfanyl)-4-(substituted phenyl)-6-methyl-1,4-dihydro-5-pyrimidine carboxamides (1-30) were designed and synthesized keeping in view the structural requirements as suggested in the pharmacophore model for antihypertensive activity. All the synthesized compounds were tested for antihypertensive activity by non-invasive blood pressure (NIBP) measurements (tail-cuff method) in rats. Almost all the tested compounds displayed considerable decrease in the blood pressure as compared to control. Thirteen compounds showed significant antihypertensive activity comparable to the standard drug nifedipine. (C) 2010 Elsevier Masson SAS. All rights reserved.