抗甲状腺药物丙硫氧嘧啶的硒类似物的合成及其抗过氧化物酶活性

Synthesis and the antiperoxidase activity of seleno analogues of the antithyroid drug propylthiouracil.

作者信息

Aboul-Enein H Y, Awad A A, al-Andis N M

机构信息

Bioanalytical and Drug Development Laboratory, MBC-03 King Faisal Specialist Hospital and Research Centre, Riyadh, Kingdom of Saudi Arabia.

出版信息

J Enzyme Inhib. 1993;7(2):147-50. doi: 10.3109/14756369309040756.

DOI:10.3109/14756369309040756

PMID:7509869

Abstract

The synthesis of 6-n-propyl-2-selenouracil (PSeU, Ib) and its methyl derivative (MSeU, Ic) are described. Replacement of the sulfur atom at C2 by selenium increased with antiperoxidase activity of these analogues five fold when compared to the clinically used antithyroid drug propylthiouracil (PTU). The structure-activity relationships of these agents are discussed.

摘要

描述了6-正丙基-2-硒脲嘧啶（PSeU，Ib）及其甲基衍生物（MSeU，Ic）的合成。与临床使用的抗甲状腺药物丙硫氧嘧啶（PTU）相比，这些类似物中C2位的硫原子被硒取代后，其抗过氧化物酶活性提高了五倍。讨论了这些药物的构效关系。