Some structural changes on triazolyl-benzotriazoles and triazolyl-benzimidazolones as potential potassium channel activators. III

被引：29
作者：
Biagi, G
Calderone, V
Giorgi, I
Livi, O
Scartoni, V
Baragatti, B
Martinotti, E
机构：
[1] Univ Pisa, Dipartimento Sci Farmaceut, I-56126 Pisa, Italy
[2] Univ Pisa, Dipartimento Psiciat Neurobiol Farmacol & Biotecn, I-56126 Pisa, Italy
来源：
FARMACO | 2001年 / 56卷 / 11期
关键词：
1,2,3-triazoles; benzimidazolones; benzotriazoles; benzotriazin-4-ones; potassium channels;
D O I：
10.1016/S0014-827X(01)01148-X
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
This paper reports the synthesis and pharmacological evaluation of some compounds, obtained by structural modifications of 1,2,3-triazolyl-benzotriazoles and 1,2,3-triazolyl-benzimidazolones, which had shown activity as potential activators of the big-conductance calcium-activated potassium channels (BKCa). Changes have concerned the introduction of a hinderer substituent in the 5-position of-the benzimidazolone (4a, b) and benzotriazole (5a, b) rings, opening of the benzimidazolone ring (7) and substitution of the 1,2,3-triazole ring with a 2-hydroxyphenyl ring (10). Furthermore a series of 3-aryl-benzotriazin-4-one derivatives (13a-e) has been studied, which appears as a modification and/or combination of the benzimidazolone and benzotriazole rings. Only compound 10 shows interesting activity, while the other structural modifications either do not increase (compounds 4 and 5) or reduce (compounds 7 and 13) the pharmacological activity. However, these results provide useful information about structure-activity relationships. (C) 2001 Elsevier Science S.A. All rights reserved.
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收藏
页码：841 / 849
页数：9
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