Steroid Acid Amides of Diamino Diphenyl Sulfone

¹ Director, Bacteriology Department, Sea View Hospital.

A series of steroid acid amides of diamino diphenyl sulfone was synthesized and explored for chemotherapeutic activity.

4-desoxycholylamino 4'-amino diphenyl sulfone (B111), a representative member of this new group of compounds was tolerated in large amounts by experimental animals without toxic symptoms when administered orally or intravenously.

It was active in vitro on "wild" and laboratory strains of Myco. tuberculosis and active in vivo in experimental animal tuberculosis in the range of diamino diphenyl sulfone and other, but, toxic derivatives of DDS.

Activity of B111 was due to the unhydrolized compound as documented by infra red spectral comparisons. The steroid moiety of the compound appears to act simultaneously as a detoxifier and a chemotherapeutic activator.

In mixtures with streptomycin, synergism with striking bacteriostatic and bactericidal effects on Myco. tuberculosis was observed.

In a preliminary clinical study, the administration of large doses of B111 was perfectly tolerated by humans.