Syntheses and Antihypertensive Activities of 1,4-Dihydropyridine-5-phosphonate Derivatives. III(Medicinal Chemistry,Chemical)

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Various 1- and 2-substituted and 1,2-fused 1,4-dihydropyridine-5-phosphonate derivatives were designed and synthesized as analogues of 1,4-dihydropyridine-3,5-dicarboxylate, and their antihypertensive activities were examined. Several compounds proved to be equal or superior to nifedipine in lowering blood pressure in normotensive and spontaneously hypertensive rats. Among these compounds, 1-substituted 1,4-dihydropyridine derivatives showed potent antihypertensive activities. The structure-activity relationships are discussed.

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