Synthesis of 4-(Carbonyloxyphenyl)-1,4-dihydropyridines as potential antihypertensive agents

Bansal, R. and Narang, G. and Calle, C. and Carron, R. and Pemberton, K. and Harvey, A.L. (2013) Synthesis of 4-(Carbonyloxyphenyl)-1,4-dihydropyridines as potential antihypertensive agents. Drug Development Research, 74 (1). pp. 50-61. ISSN 0272-4391 (https://doi.org/10.1002/ddr.21056)

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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.