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Abstract
The synthesis of four fluorinated-2 thiouracil derivatives, namely, 6-trifluoromethyl* -2-thiouracil, l-methyl-6-trifluoromethyl-2-thiouraci1, l-acetyl-6-trifluoromethyl-2-thiouracil and 6-n-heptafluoropropyl-2-thiou-racil was achieved. 6-n-Heptafluoropropyl-2-thiouracil displayed higher antithyroid activity followed by 6-trifluoromethyl derivative and 1-methyl-6-trifluoromethyl analogue when compared to 6-n-propyl-2-thiouracil. 1-Acetyl 6-trifluoromethyl-2-thiouracil exhibited no antithyroid activity. The structure-activity relationships (SAR) of this class of compounds are discussed.