SYNTHESIS AND ANTITHYROID ACTIVITY OF FLUORINATED 2-THIOURACIL ANALOGS

被引：4

作者：

ABOULENEIN, HY ^{[1
]}

ALANDIS, NM ^{[1
]}

机构：

[1] KING SAUD UNIV,COLL SCI,DEPT ORGAN CHEM,RIYADH 11405,SAUDI ARABIA

来源：

JOURNAL OF ENZYME INHIBITION | 1993年 / 7卷 / 03期

关键词：

FLUORINATED ANALOGS OF PROPYLTHIOURACIL; ANTITHYROID ACTIVITY; ANTIPEROXIDASE ACTIVITY; STRUCTURE-ACTIVITY RELATIONSHIPS;

D O I：

10.3109/14756369309040762

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The synthesis of four fluorinated-2-thiouracil derivatives, namely, 6-trifluoromethyl-2-thiouracil, 1-methyl-6-trifluoromethyl-2-thiouracil, 1-acetyl-6-trifluoromethyl-2-thiouracil and 6-n-heptafluoropropyl-2-thiouracil 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.

引用

页码：197 / 202

页数：6

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