CHEMOTHERAPEUTIC STUDIES OF 4-AMINO-4'-PROPYLAMINODIPHENYLSULFONE ALONE AND IN COMBINATION WITH SULFADIAZINE IN EXPERIMENTAL PNEUMOCOCCUS INFECTION

¹ Division of Physiology, National Institute of Health, Bethesda, Md.

The toxicity and chemotherapeutic activity of 4-amino-4'-n-propylaminodiphenylsulfone have been studied in experimental pneumococcus I infection in mice in comparison with the parent substance,4,4'-diaminodiphenylsulfone, and with sulfadiazine.

The n-propyl derivative retains a moderate chemotherapeutic activity, not as great however as that of 4,4'-diaminodiphenylsulfone. The aminopropyl derivative is tolerated in normal animals in much larger doses, weight for weight, than the parent sulfone, thus giving it a better chemotherapeutic index; and this appears to be accounted for wholly or in part by the fact that it is not as well absorbed as the parent compound. In very large doses, divided over several days, the aminopropyl compound appears to be more toxic for infected mice than for normal mice. It is not as effective as sulfadiazine on oral administration, and is less well tolerated in large doses in infected animals.

The simultaneous administration of small doses of sulladiazine and the npropyl derivative gave a degree of chemotherapeutic effectiveness greater than the sum of effects from the individual components.