アミノアルコール誘導体の研究(第4報)3-ジアルキルアミノ-1,2-エポキシプロパンのN, N-ジアルキル脂肪酸アミドによる開裂反応生成物および安息香酸誘導体の薬理学的研究

概要

論文の詳細を見る
In order to investigate the relation between chemical structure and the pharmacological activity, N, N-dialkylcarbamoyldialkylamino alcohols and benzoate derivatives were synthesized. Twenty-three substances were examined for local anesthetic activity, antispasmodic activity, inhibitory activity on writhing syndrome produced by acetic acid and analgesic activity on pain produced by hot plate. In general, pharmacological activity of N, N-dialkylcarbamoyldialkylamino alcohols was stronger than that of dialkylamino alcohols. 1-(N, N-diethyl)-4-dibutyl-3-butanol hydrochloride (IIf) showed duration of topical anesthesia almost equal to cocaine and 1-(N, N-dibutyl) carbamoyl-4-piperidino-3-butanol hydrochloride (IIl) showed activity of infiltration anesthesia about 2.5-3.5 times that of lidocaine. 1-(N, N-Dibutyl) carbamoyl-4-dibutylamino-3-butanol hydrochloride (IIg) showed several times as potent an analgesic activity as pyrabital in the hot plate method.
公益社団法人日本薬学会の論文
1977-10-25