1953 年 73 巻 7 号 p. 729-732
In order to obtain local anesthetics which are not antagonized by sulfanilamides, various substances possessing thioalkyl group in the nucleus as the anesthesis-strengthening group were synthesized. The pharmaceutical efficacy of some of the promising of these compounds was determined. Surface anesthetic power was tested on rabbit cornea and irritation on aural canal of a guinea pig, infiltrating anesthetic power by human subcutis and rabbit eye lid, and the lethal dose, LD50, by mouse. As a result, it was found that the introduction of S-alkyl group extremely heightened the rate in alkamine and dialkylaminoacetanilide types while such an increase was not observed in amidine type, although the infiltrating anesthetic power in the latter was strengthened. The compounds showing a large pharmaceutical efficacy rate were diethylaminoethyl p-thioethylcinnamate and diethylamino ethyl 3-thioethyl-4-hydroxybenzoate which were respectively 5 and 3 times that of procaine and 20 and 7 times that of cocaine. p-Thioisoamyl diethylamino acetanilide possessed a small minimum concentration, showing surface anesthetic power even in 0.1% concentration, and was slightly better than cocaine.