Benzylpiperazine Derivatives. II. Syntheses and Cerebral Vasodilating Activities of 1-[(3-Alkyl-3-hydroxy-3-phenyl)propyl]-4-benzylpiperazine Derivatives(Medicinal Chemistry,Chemical)

概要

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Analogs of 1-[(3-alkyl-3-hydroxy-3-phenyl)propyl]-4-(2,3,4-triniethoxybenzyl)piperazine (1) were prepared and tested for cerebral vasodiiating activity. It was found that the potency depends positively on the number of methoxyl groups on the benzyl moiety, and the homopiperazine analogs seem to be equipotent to the corresponding piperazines. From the standpoints of potency and ease of synthesis, 8k was selected for further study. Further analogs, which have various substituents in place of the benzyl moiety of 8k, were prepared and tested for cerebral vasodiiating activity. These analogs were less potent than 8k. It was suggested that the benzyl moiety of 8k plays an important role in the high cerebral vasodiiating activity.
公益社団法人日本薬学会の論文
1987-07-25