Trypanocidal and Spirochetocidal Compounds Derived from BAL and Organic Arsenicals

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Abstract
Chemotherapeutic activity of organo-metallic compounds was studied in combination with dithiols. The condensation product of oxophenarsine and BAL, 2-amino-4-[methylol-(ethylenedimercaptoarsino)]-phenol, (I), and its hydrochloride, (II), were synthesized and found to combine relatively low toxicity with significant trypanocidal and spiro-chetocidal activity. In rabbits 0.05 g./kg. of I is tolerated, while 0.08 g./kg. is lethal. In tests on 16 cases of rabbit syphilis 0.006 g./kg. of I had an immediate spirochetocidal effect. The intraperit. max. tolerated dose of II in mice is 0.12 g./kg. The min. curative dose of II in Trypanosoma equiperdum infection of the mouse is 0.02 g./kg. Similar results were obtained with analogous BAL derivs. of other aromatic arsenicals as well as antimonials. The mechanism of chemotherapeutic activity includes a factor which is a function of the distr. of the chemotherapeutic agent within the organism. Since combination with BAL and BAL derivs. affects solubility characteristics and hence distr., repercussions on the chemotherapeutic spectrum are to be expected for such BAL derivs. as compared with the parent organo-metallics. The solubility of organo-metallics may be modified at will by suitable choice of the dithiol components, such as the original BAL, an alcohol, or its carboxylic acid and ethyl ether derivatives.

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