1953 年 73 巻 7 号 p. 725-728
In order to find out the influence of the S-alkyl group on the effect, 7 kinds of N, N′-disubstituted benzamidines, 4 kinds of N, N-disubstituted benzamidines, and 14 kinds of naphthoamidines, all possessing a thioalkyl group, were synthesized. Preparation of N, N′-disubstituted compounds was carried out by the halogenation and amination of the corresponding thioalkylbenzoic acid alkylamides, and the N, N-compounds by the Grignard reaction of the corresponding benzonitriles. The hydrochlorides of the former were of low hydrophilic properties when the alkyl in N and N′ were of aromatic nucleus and were assumed to be unsuitable as local anesthetics. On the other hand, the physical properties of the N, N-disubstituents were found to be more suitable for such application. Their pharmacological actions are shown in Report V.