2-Alkyloxyalkylthiohypoxanthines as new potent inhibitors of xanthine oxidase

被引:27
作者
Biagi, G [1 ]
Giorgi, I [1 ]
Pacchini, F [1 ]
Livi, O [1 ]
Scartoni, V [1 ]
机构
[1] Univ Pisa, Dipartimento Sci Farmaceut, I-56100 Pisa, Italy
来源
FARMACO | 2001年 / 56卷 / 11期
关键词
xanthine oxidase; inhibitors; 2-thiohypoxanthine; 2-mercaptohypoxanthine; 2-thioxo-1,2,3,7(9)-tetrahydro-purin-6-one;
D O I
10.1016/S0014-827X(01)01160-0
中图分类号
R9 [药学];
学科分类号
1007 [药学];
摘要
The title compounds were prepared and tested as xanthine oxidase (XO) inhibitors. Results evidenced that potency was related to the position of the oxygen atom in the 2-linear chain and that it grew with distance from the sulfur atom until it became equipotent to 2-n-hexylthiohypoxanthine. Enzymatic oxidation on C(2) occurred in the 8-alkylthiohypoxanthines. On the contrary, oxidation on C(8) did not occur in the 2-alkythioderivatives, demonstrating that the chain forced these molecules to form a complex with molybdenum(VI) involving only the N(3) and N(9) nitrogen atoms. (C) 2001 Elsevier Science S.A. All rights reserved.
引用
收藏
页码:809 / 813
页数:5
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