Chemotherapy of bacterial infections. Part III. Synthesis of (N⁴)-amino-substituted heterocyclic derivatives of sulphanilamide

Abstract

The synthesis of thirteen (N⁴) amino-substituted sulphanilamide compounds of thiozal and related derivatives is described. None of them showed any activity in experimental streptococcal and pneumococcal infections in mice. Five sulphanilamide derivatives of acridine of the above group have also been described. Though some of them possessed considerable activity in the streptococcal infections, they were inactive in pneumococcal infections. It is apparent that for pronounced antibacterial action the heterocyclic ring should be substituted in the sulphonamide radical leaving a free amino group, which appears to play some significant, but as yet not perfectly understood, role in the mechanism of therapeutic action.