Zusammenhänge zwischen chemischer Konstitution und Antitrypsinwirkung bei Derivaten der 4-Aminomethyl-benzoesäure und anderen strukturverwandten cyclischen Verbindungen

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Abstract
The molecule of 4-aminomethyl-benzoic acid, which was shown to be an inhibitor of trypsin in a previous publication, was systematically modified. The antitrypsin activity of the derivatives obtained was studied on the basis of the tryptic activation of chymotrypslnogen and the tryptic hydrolysis of casein. In addition to the already known relationship between chemical structure and antitrypsin activity of this type of compound, it was also found that esters and amides of 4-aminomethylbenzoic acid and of other cyclic aminocarboxylic acids are especially powerful inhibitors of trypsin. The benzyl esters of 4-aminomethyl-benzoic acid and of benzamidine-4-carboxylic acid inhibit trypsin several times more strongly than the hitherto known inhibitors of low molecular size.