STUDIES ON THERAPEUTIC AGENTS IN LEPROSY THE EFFECT OF ACETYLATED DDS

Abstract

The majority of the therapeutic agents of the DDS series are those with an aromatic ring attached to 4-aminophenylsulfone and the amino radical in the 4 position is considered important from the standpoint of therapeutic effect. It is known that when the amino on both sides of DDS replaced with the acetyl radical, there is a great difference thrapeu-tically. The toxicity is reduced but at the same time, the effect should also be affected. As 4, 4' diacetaminodiphenylsulfone has been found to be effective against pneumococci and streptococci it can be assumed that it is converted to an effective form in the body. The mechanism of action was therefore investigated.
Deacetylization was first studied by extracting the urine and blood of subjects given the agent with ethyl acetate and subjecting the extract to paper electrochromatography. DDS and monoacetate were proven.
The same procedure was carried out in the DDS administered subject and monoacetate was shown to be present. Similar results were obtained with mouse liver.
The pharmacological actions of DDS, the monoacetate and the diacetate were compared. It was found that the toxicity of the latter two was far weaker than that of DDS. It was also found that DDS paralyzes the peripheral endings of the parasympathetic nerves which accelerate intestinal motility, causes a rise in blood pressure and stops the pulsation of the toad heart in systole in a dose of 20*50mg/20cc whereas the latter two agents do not have these actions. On the basis of these results, it was decided that 4, 4'-diacetaminodi-phenylsulfone could be safely used clinically and it was applied in 10 cases of leprosy. It was found that this agent was effective. It is suggested that 4, 4'-diacetaminodiphenyl-sulfone will be useful in cases in which DDS or Promin cannot be to related or in those in which there is no longer any response to Promin or DDS.