Synthesis of 3-benzyl-2-substituted quinoxalines as novel monoamine oxidase A inhibitors

被引：64
作者：
Hassan, SY
Khattab, SN
Bekhit, AA [1 ]
Amer, A
机构：
[1] Univ Alexandria, Fac Sci, Dept Chem, Alexandria 21521, Egypt
[2] Univ Alexandria, Fac Pharm, Dept Pharmaceut Chem, Alexandria 21521, Egypt
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 06期
关键词：
MAO-A inhibitors; 3-benzyl-2-substituted quinoxalines;
D O I：
10.1016/j.bmcl.2005.11.088
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A new series of 3-benzyl-2-substituted quinoxalines have been synthesized by means of microwave enhancement of nucleophilic substitution reaction involving the corresponding 2-chloroquinoxaline analogs and substituted amines or hydrazine. The synthesized compounds were evaluated for their monoamine oxidase A and B inhibitory activity by determination of their IC50. All the newly synthesized compounds showed more selective inhibitory activity toward NIAO-A than MAO-B. In addition, the acute toxicity of the synthesized compounds was determined. This work may be a fruitful matrix of the synthesis of a new series of novel MAO-A inhibitors with good safety margins. (C) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1753 / 1756
页数：4
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