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Journal of Pharmacology And Experimental Therapeutics, Vol. 85, Issue 2, 129-139, 1945
Copyright © 1945 by American Society for Pharmacology and Experimental Therapeutics

ANTITHYROID STUDIES

III. THE GOITROGENIC ACTIVITY OF CERTAIN CHEMOTHERAPEUTICALLY ACTIVE SULFONES AND RELATED COMPOUNDS

D. A. McGINTY 1 and W. G. BYWATER 1

1 From the Research Laboratories, Parke, Davis and Company, Detroit, Michigan

Thirty eight compounds including 14 chemotherapeutically active sulfones and sulfides, were tested for their antithyroid activity in rats. Promizole was the most active goitrogen of the sulfone group, having, however, only 18 per cent of the activity of thiouracil. In general, sulfides corresponding to the sulfones were more active, "Promizole sulfide" showing 53 per cent of the potency of thiouracil.

Of the simple heterocycles related to the above compounds only 5-aminothiadiazole-2-thiol (TC-68) exhibited marked antithyroid activity and is being investigated further. Certain relationships between chemical structure and antithyroid activity of these simple heterocyclic compounds have been discussed in terms of the experimental data.

Submitted on June 18, 1945




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 Arch Intern MedHome page
R. H. WILLIAMS and G. A. KAY
THIOURACILS AND THIOUREAS: Comparisons of the Absorption, Distribution, Destruction and Excretion
Arch Intern Med, July 1, 1947; 80(1): 37 - 52.
[Abstract] [PDF]


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Copyright © 1945 by the American Society for Pharmacology and Experimental Therapeutics.