SYNTHESIS AND ANTIALLERGIC ACTIVITY OF DIMETHYL-2-(PHENYLCARBAMOYL)ETHYLSULFONIUM P-TOLUENESULFONATE DERIVATIVES

The derivatives of dimethyl-2-(phenylcarbamoyl)ethylsulfonium p-toluen esulfonates were synthesized and evaluated for antiallergic activity. The 2,3-dihydroxyethoxy group was introduced to the phenyl ring from t he standpoint of lipophilicity and electronic effects of substituent. The IgE-induced rat passive cutaneous anaphylaxis (PCA) was inhibited by oral administration of several substituted [(4-propoxyphenyl)carbam oyl]ethyldimethylsulfonium p-toluenesulfonate derivatives. Among them xypropoxy)phenyl]-carbamoyl]ethyldimethylsulfonium p-toluenesulfonate (1a, IPD-1151T) was found to possess considerable activity in the PCA test, and it was launched as Suplatast tosilate in Japan.