Synthesis, human monoamine oxidase inhibitory activity and molecular docking studies of 3-heteroarylcoumarin derivatives.

Delogu G; Picciau C; Ferino G; Quezada E; Podda G; Uriarte E; Vina D

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Synthesis, human monoamine oxidase inhibitory activity and molecular docking studies of 3-heteroarylcoumarin derivatives.

机译：3-杂芳基香豆素衍生物的合成，人单胺氧化酶抑制活性和分子对接研究。

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Monoamine oxidase (MAO) is an important drug target for the treatment of neurological disorders. Series of 3-indolyl and 3-thiophenylcoumarins were synthesized and evaluated as inhibitors of the two human MAO isoforms, hMAO-A and hMAO-B. In general, the derivatives were found to be selective hMAO-B inhibitors with IC(50) values in the nanoMolar (nM) to microMolar (muM) range. Docking experiments were carried out in order to compare the theoretical and experimental affinity of these compounds to the hMAO-B protein. According to our results, docking experiments could be an interesting approach to try to predict the activity of this class of coumarins against MAO-B receptors.

机译：单胺氧化酶（MAO）是治疗神经系统疾病的重要药物靶标。合成了一系列的3-吲哚基和3-硫代苯基香豆素，并将其评估为两种人MAO同种型hMAO-A和hMAO-B的抑制剂。通常，发现这些衍生物是选择性hMAO-B抑制剂，IC（50）值在纳摩尔（nM）至微摩尔（muM）范围内。为了比较这些化合物对hMAO-B蛋白的理论和实验亲和力，进行了对接实验。根据我们的结果，对接实验可能是一种有趣的方法，可以尝试预测此类香豆素对MAO-B受体的活性。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2011年第4期|共6页
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Delogu G; Picciau C; Ferino G; Quezada E; Podda G; Uriarte E; Vina D;
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1. Synthesis, human monoamine oxidase inhibitory activity and molecular docking studies of 3-heteroarylcoumarin derivatives. [J] . Delogu G, Picciau C, Ferino G, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2011,第4期

机译：3-杂芳基香豆素衍生物的合成，人单胺氧化酶抑制活性和分子对接研究。
2. Flavonoids from Sideritis Species: Human Monoamine Oxidase (hMAO) Inhibitory Activities, Molecular Docking Studies and Crystal Structure of Xanthomicrol [J] . Turkmenoglu Fatma Pinar, Baysal Ipek, Ciftci-Yabanoglu Samiye, Molecules . 2015,第5期

机译：铁皮炎物种的类黄酮：人单胺氧化酶（hMAO）抑制活性，分子对接研究和Xanthomicrol的晶体结构。
3. Flavonoids from Sideritis Species: Human Monoamine Oxidase (hMAO) Inhibitory Activities, Molecular Docking Studies and Crystal Structure of Xanthomicrol [J] . #x130, hsan #xC7, al#x131, Molecules . 2015,第5期

机译：铁皮炎物种的类黄酮：人单胺氧化酶（hMAO）抑制活性，分子对接研究和Xanthomicrol的晶体结构。
4. Docking and molecular dynamics study on the inhibitory activity of coumarins to aldose reductase [C] . Zhiguo Wang, Baoping Ling, Rui Zhang, 第四届国际分子模拟与信息技术应用学术会议（The 4th International Conference of Molecular Simulations and Applied Informatics Technologies）论文集 . 2008

机译：香豆素对醛糖还原酶抑制作用的对接和分子动力学研究
5. Expression and functional characterization of monoamine oxidase from the zebrafish (Danio rerio): Comparisons with human monoamine oxidases A and B. [D] . Kacar, Betul. 2009

机译：斑马鱼（Danio rerio）单胺氧化酶的表达和功能表征：与人单胺氧化酶A和B的比较。
6. Flavonoids from Sideritis Species: Human Monoamine Oxidase (hMAO) Inhibitory Activities Molecular Docking Studies and Crystal Structure of Xanthomicrol [O] . Fatma Pinar Turkmenoglu, İpek Baysal, Samiye Ciftci-Yabanoglu, 2015

机译：黄体激素类黄酮：人单胺氧化酶（hMAO）抑制活性分子对接研究和Xanthomicrol的晶体结构。
7. Flavonoids from Sideritis Species: Human Monoamine Oxidase (hMAO) Inhibitory Activities, Molecular Docking Studies and Crystal Structure of Xanthomicrol [O] . Fatma Pinar Turkmenoglu, İpek Baysal, Samiye Ciftci-Yabanoglu, 2015

机译：来自sideritis物种的黄酮类化合物：人单胺氧化酶（hmaO）抑制活性，分子对接研究和Xanthomicrol的晶体结构

Synthesis, human monoamine oxidase inhibitory activity and molecular docking studies of 3-heteroarylcoumarin derivatives.

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