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Synthesis of 4‐(Carbonyloxyphenyl)‐1,4‐Dihydropyridines as Potential Antihypertensive Agents
Authors:Ranju Bansal  Gaurav Narang  Carmen Calle  Rosalia Carron  Karen Pemberton  Alan L. Harvey
Affiliation:1. University Institute of Pharmaceutical Sciences, Panjab University, , Chandigarh, 160014 India;2. Departamento de Fisiología y Farmacología, Facultad de Farmacia, Campus “Miguel de Unamuno”, , E‐37007 Salamanca, Spain;3. Thistle Technologies, , Branford, CT, 06405 USA;4. Strathclyde Institute for Drug Research, Department of Physiology and Pharmacology, University of Strathclyde, , Glasgow, G4 0NR UK
Abstract:
Preclinical Research
A series of novel symmetric and asymmetric 4‐(carbonyloxyphenyl)‐1,4‐dihydropyridines (DHPs) was synthesized and evaluated for calcium channel blocking, vasodilatory and antihypertensive properties. Some of these new DHPs displayed potent calcium channel blocking and good vasodilatory activities. Heart rate remained relatively constant in comparison with blood pressure changes in the case of these newly synthesized compounds, thereby decreasing the probability of reflex tachycardia, a major side effect of nifedipine. The most potent compound, ethyl methyl 4‐(3‐isopropylcarbonyloxyphenyl)‐2,6‐dimethyl‐1,4‐dihydropyridine‐3,5‐dicarboxylate (14c) exhibited antihypertensive activity comparable with the standard drug—nifedipine.
Keywords:calcium channel blockers  1  4‐dihydropyridines  vasodilators  antihypertensive activity  Hantzsch synthesis
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