Synthesis and Antihypertensive Activities of 1, 4-Dihydropyridine-5-phosphonate Derivatives. II

A series of 1, 4-dihydropyridine-5-cyclic phosphonate derivatives, designed as analogues of 1, 4- dihydropyridine-3, 5-dicarboxylate calcium antagonists, was synthesized and examined for antihypertensive activity. Several compounds were proved to have activities superior or comparable to that of nif...

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Published inChemical & pharmaceutical bulletin Vol. 35; no. 10; pp. 4144 - 4154
Main Authors MORITA, IWAO, KUNIMOTO, KATSUTOSHI, TSUDA, MASAMI, TADA, SHIN-ICHI, KISE, MASAHIRO, KIMURA, KIYOSHI
Format Journal Article
LanguageEnglish
Published Tokyo The Pharmaceutical Society of Japan 1987
Maruzen
Japan Science and Technology Agency
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Summary:A series of 1, 4-dihydropyridine-5-cyclic phosphonate derivatives, designed as analogues of 1, 4- dihydropyridine-3, 5-dicarboxylate calcium antagonists, was synthesized and examined for antihypertensive activity. Several compounds were proved to have activities superior or comparable to that of nifedipine in lowering blood pressure in normotensive and spontaneously hypertensive rats (SHR). Among these compounds, methyl 2, 6-dimethyl-5- (2-oxo-1, 3, 2-dioxaphosphorinan-2-yl) -4- (2-nitrophenyl) -1, 4-dihydropyridine-3-carboxylate (31, DHP-218) was approximately 7 times more active than nifedipine in SHR and was selected for further development and clinical evaluation. The structure-activity relationships are discussed.
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ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.35.4144