کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1397566 | 1501178 | 2011 | 6 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Synthesis, human monoamine oxidase inhibitory activity and molecular docking studies of 3-heteroarylcoumarin derivatives Synthesis, human monoamine oxidase inhibitory activity and molecular docking studies of 3-heteroarylcoumarin derivatives](/preview/png/1397566.png)
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 IC50 values in the nanoMolar (nM) to microMolar (μM) 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.
Three series of 3-heteroarylcoumarin derivatives have been synthesized and evaluated as hMAO inhibitors. The biological data were compared to the molecular docking study.Figure optionsDownload as PowerPoint slideResearch highlights
► Synthesis of 3-heteroarylcumarins.
► Evaluation of hMAO activity.
► Docking studies.
► Prediction of hMAO-B activity for new derivatives.
Journal: European Journal of Medicinal Chemistry - Volume 46, Issue 4, April 2011, Pages 1147–1152