Syntheses and Antihypertensive Activities of 1, 4-Dihydropyridine-5-phosphonate Derivatives. III

IWAO MORITA; Yuko HARUTA; TOSHIO TOMITA; MASAMI TSUDA; KAZUHISA KANDORI; MASAHIRO KISE; KIYOSHI KIMURA

doi:10.1248/cpb.35.4819

IWAO MORITA, Yuko HARUTA, TOSHIO TOMITA, MASAMI TSUDA, KAZUHISA KANDORI, MASAHIRO KISE, KIYOSHI KIMURA

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Keywords: 1, 4-dihydropyridine derivative, phosphonate derivative, 1, 2-fused 1, 4-dihydropyridine, calcium antagonist, antihypertensive activity, nifedipine, structure-activity relationship

JOURNAL FREE ACCESS

1987 Volume 35 Issue 12 Pages 4819-4828

DOI https://doi.org/10.1248/cpb.35.4819

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Abstract

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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