Chemotherapy of bacterial infections Part II. Synthesis of some sulphanilamide derivatives and the relation of chemical constitution to chemotherapeutic action

Abstract

The synthesis and the chemotherapeutic effects in experimental streptococcal and pneumococcal infections in mice of new sulphanilamide derivatives are described. 2-N¹ sulphanilamidothiazol appears to possess a very striking effect in these infections. The realtionship of chemical constitution to chemotherapeutic action in this group of compounds has been outlined basing on a study of the therapeutic properties of about 500 compounds till now reported. While the substitution at the amino radical of sulphanilamide does not produce compounds of increased activity but only suppress the polyvalent action of the original compound, the substitution at the amide part of the molecule, especially by a heterocyclic ring, produces compounds of increased activity, particularly in infections in which sulphanilamide is very little effective. The highly active diaminodiphenylsulphone derivatives have to be properly modified to be used in practical therapy. There does appear to be a sort of specificity of the compounds towards different types of infections so that the new compounds produced should be tested in different types of infections also.