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Journal of Pharmacology And Experimental Therapeutics, Vol. 70, Issue 2, 221-227, 1940
Copyright © 1940 by American Society for Pharmacology and Experimental Therapeutics

THE TOXICITY, TREPONEMICIDAL ACTIVITY, AND POTENTIAL THERAPEUTIC UTILITY OF SUBSTITUTED PHENYLARSENOXIDES III. MONOSUBSTITUTED COMPOUNDS: ACIDS, ESTERS, BENZOPHENONE, METHYLSULFONE

HARRY EAGLE 1, RALPH B. HOGAN 1, GEORGE O. DOAK 1, and HARRY G. STEINMAN 1

1 From the United States Public Health Service, Washington, D.C., and the Syphilis Division of the Department of Medicine, Johns Hopkins Medical School, Baltimore, Md.

The relative treponemicidal activity in vitro and toxicity in white mice have been determined for o-, m-, and p-COOH, o- and p-SO3Na, p-OCH2COOH, p-CH=CHCOOH, p-CH2COOH, p-(CH2)2COOH, p-(CH2)3COOH, p-NHCO(CH)2COOH, m-COOC2H5, p-COOC2H5, p-COC6H5, p-COCH3, and p-SO2CH3 phenylarsenoxides. In general, mono-substitution with an acidic group markedly inhibited the activity and decreased the potential therapeutic utility of phenylarsenoxide. The mechanism of that inhibition is discussed in the text.

Blocking the acidic group, either by esterification, or as in the acetophenone, benzophenone and methylsulfone compounds, largely removed the inhibitory effect of the acid on treponemicidal activity, and with two of the compounds resulted in a ratio of treponemicidal activity:toxicity significantly exceeding that of phenylarsenoxide.

Submitted on May 13, 1940






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