Long-acting dihydropyridine calcium antagonists. 1. 2-Alkoxymethyl derivatives incorporating basic substituents

JE Arrowsmith, SF Campbell, PE Cross…

文献索引：Arrowsmith; Campbell; Cross; Stubbs; Burges; Gardiner; Blackburn Journal of Medicinal Chemistry, 1986 , vol. 29, # 9 p. 1696 - 1702

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被引用次数: 282

摘要

A series of dihydropyridines substituted at the 2-position by basic side chains are described and their potencies as calcium antagonists listed. One compound, 24 (2-aminoethoxy) methyl]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1, 4dihydropyridine (17, amlodipine) was found to be comparable in potency to nifedipine and to have an elimination half-life of 30 h in dogs. Oral bioavailability approached 100%, and ...