H. Barrett, F. Gassner, K. Dittmer
Feb 1, 1951
Citations
0
Influential Citations
9
Citations
Journal
Endocrinology
Abstract
IN A previous paper (Barrett, Goodman, Dittmer, 1948), the synthesis of 5-halogeno-2-thiouracil and of 6-methyl-5-iodo-2-thiouracil was described. Three derivatives were found to possess antithyroid activity as measured by their ability to increase thyroid weight in the rat and to decrease thyroid iodine. A fuller investigation has now been made, and we wish here to give a more detailed account of their antithyroid behavior. One of the purposes we hoped to achieve in the synthesis of these compounds was that of providing an antithyroid drug which might render unnecessary the simultaneous use of iodine and thiouracil as practiced preoperatively in patients with hyperthyroidism, and which might alleviate certain undesirable clinical defects in thiouracil or in its 6-alkyl derivatives (Christian, 1946). Interest naturally centered around the 5-iodo derivative, as it would be composed of a presumed antithyroid moiety plus an essential thyroid metabolite.