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

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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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