ANTITHYROID STUDIES. I. THE GOITROGENIC ACTIVITY OF SOME THIOUREAS, PYRIMIDINES AND MISCELLANEOUS COMPOUNDS

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

A group of 56 compounds have been tested for their ability to inhibit the function of the thyroid gland. The relative activity of these compounds has been determined by comparison with thiouracil using as a base the dose of the latter needed to reduce the thyroid iodine to 12 mg. per cent when the drug is administered to rats in the food for a ten day period. The relationship between the dose and the thyroid iodine concentration is a linear one for those compounds tested at several dose levels and it is postulated that other compounds will also give straight-lines having the same slope when the thyroid iodine concentration is plotted against dose. This assumption affords a practical means of determining the relative activities of comparable compounds

The thioureas tested were less active than thiouracil. Similarly, the thiobarbituric acids investigated were also less active except 5,5-diethyl-2-thiobarbituric acid.

Of the miscellaneous compounds subjected to test, pyridine-2-thiol, thiazoline-2-thiol and benzimidazole-2-thiol were found to be the most active. The latter two have been tested at several dose levels and found to be more effective than thiouracil in the rat. Derivatives of these compounds and of pyridine-2-thiol are being investigated further.

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				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]