新型单胺氧化酶A抑制剂3-苄基-2-取代喹喔啉的合成
Synthesis of 3-benzyl-2-substituted quinoxalines as novel monoamine oxidase A inhibitors.
作者信息
Hassan Seham Y, Khattab Sherine N, Bekhit Adnan A, Amer Adel
机构信息
Department of Chemistry, Faculty of Science, University of Alexandria, Alexandria 21521, Egypt.
出版信息
Bioorg Med Chem Lett. 2006 Mar 15;16(6):1753-6. doi: 10.1016/j.bmcl.2005.11.088. Epub 2005 Dec 13.
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 IC(50). All the newly synthesized compounds showed more selective inhibitory activity toward MAO-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.
通过微波增强亲核取代反应，利用相应的2-氯喹喔啉类似物与取代胺或肼合成了一系列新的3-苄基-2-取代喹喔啉。通过测定IC(50)评估了合成化合物的单胺氧化酶A和B抑制活性。所有新合成的化合物对MAO-A的抑制活性比对MAO-B更具选择性。此外，还测定了合成化合物的急性毒性。这项工作可能为合成一系列具有良好安全边际的新型MAO-A抑制剂提供丰富的基础。
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