The influence of structure and lipophilicity of hydantoin derivatives on anticonvulsant activity

被引:65
|
作者
Scholl, S [1 ]
Koch, A [1 ]
Henning, D [1 ]
Kempter, G [1 ]
Kleinpeter, E [1 ]
机构
[1] Univ Potsdam, Inst Organ Chem & Strukturanalyt, D-14415 Potsdam, Germany
关键词
Log P; hydantoins; anticonvulsant activity; RP-HPLC; pharmacophor model;
D O I
10.1023/A:1022091411018
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The lipophilicity of a representative number of hydantoin derivatives was experimentally determined by RP-HPLC. The stationary phase of RP-HPLC proved a good model to simulate effects of membrane transport. These experimental values were correlated to theoretically estimated lipophilicity values on the basis of global minima structures of the compounds studied. Both these lipophilicity and structure similarities within a proposed pharmacological model for binding the hydantoin derivatives along the sodium channel were classified with respect to their biological activity.
引用
收藏
页码:355 / 366
页数:12
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