| 谢谨 谢东升 傅磊 郭欣 何宛.D- 型氨基酸氧化酶抑制剂的发展[J].,2016,16(13):2582-2588 |
| D- 型氨基酸氧化酶抑制剂的发展 |
| Development of D-Amino Acid Oxidase Inhibitors |
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| DOI： |
| 中文关键词: D- 型氨基酸氧化酶 抗精神分裂症 镇痛 化学结构 抑制活性 构效关系 |
| 英文关键词: D-Amino acid oxidase Anti-schizophrenia Analgesia Chemcial structure Inhibitory activity Structure and activiy relationships. |
| 基金项目:高等学校博士学科点专项科研基金项目（20110073120081） |
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| 中文摘要: |
| D- 型氨基酸氧化酶(D-Amino acid oxidase，DAAO)抑制剂可以阻止D- 型氨基酸(主要是D- 型丝氨酸) 的降解和过氧化氢
的生成，在治疗精神分裂症阴性症状和认知障碍与镇痛等方面均表现出较好的疗效。从第一个DAAO抑制剂芳香羧酸类的苯甲
酸到经过烯醇互变的alpha- 羟基酮喹类抑制剂喹诺林-2,3-二酮，DAAO 抑制剂结构上总共经历了3 代变化，抑制剂与酶之间的相互
作用模式逐渐加强，其抑制活性升高了数万倍，脂溶性增加，酸性减弱，理化性质逐渐优化。本文就近10 年DAAO抑制剂的结构
发展与生物活性之间的关系进行综述。 |
| 英文摘要: |
| D-Amino acid oxidase inhibitors can prevent metabolismof D-Amino acid(D-serine) and production of hydrogen peroxide,
which can be application to anti-schizophrenia and analgesia. From the first DAAO inhibitor, benzoic acid which belongs to aromatic
carboxylic acids, to quinoxaline-2,3-diones which belongs to alpha-Hydroxyketones, DAAO inhibitors went through 3 generations with
the interaction between inhibitors and enzyme getting stronger, the activities improved more than 10 thousands, and better proper- ties,
such as higher hydrophobicity and lower acidity. In this article, we reviewed the development of DAAO inhibitors and the structure and
activity relationships in recent decade years. |
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