Abstract
Summary Nine new 1,4-dihydropyridines (DHPs) were synthesized and evaluated for their relaxant ability (rat aorta) and their antihypertensive activity in spontaneously hypertensive rats; their microsomal oxidation rate (MOR) was determined. In terms of relaxant activity, the 4-(3,5-difluorophenyl) analogues were more potent than those with 4-(4-fiuorophenyl) but weaker than those with 4-(3-nitrophenyl) substituents, while in terms of antihypertensive activity the 4-(3,5-difluorophenyl) derivatives were more potent than their 4-(3-nitrophenyl) analogues. Their MOR could be explained on the basis of the electron-withdrawing effect of the substituents, and in some cases they permitted a rationalization of discrepancies noted between DHP antihypertensive and relaxant activities. A parabolic relationship was found between the size of the carboxylic ester substituents and their contributions calculated from a Free-Wilson/Fujita-Ban analysis of relaxant activity data.
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