Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: Synthesis and pharmacological evaluation

作者：Alam Ozair^*; Khan Suroor A; Siddiqui Nadeem; Ahsan Waquar; Verma Suraj P; Gilani Sadaf J

来源：European Journal of Medicinal Chemistry, 2010, 45(11): 5113-5119.

DOI：10.1016/j.ejmech.2010.08.022

• Dihydropyrimidine
• Dihydropyridine
• DOCA-salt
• Antihypertensive activity

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.

• 出版日期2010-11