کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1397661 | 1501184 | 2010 | 9 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Inhibition of monoamine oxidase by indole and benzofuran derivatives Inhibition of monoamine oxidase by indole and benzofuran derivatives](/preview/png/1397661.png)
Monoamine oxidase (MAO) is an important drug target for the treatment of neurological disorders. A series of indole and benzofuran derivatives were synthesised and evaluated as inhibitors of the two MAO isoforms, MAO-A and MAO-B. In general, the derivatives were found to be selective MAO-B inhibitors with Ki values in the nanoMolar (nM) to microMolar (μM) concentration range. The most potent MAO-B inhibitor, 3,4-dichloro-N-(2-methyl-1H-indol-5-yl)benzamide, exhibited a Ki value of 0.03 μM and was 99 fold more selective for the B isoform. We conclude that these indole and benzofuran derivatives are promising reversible MAO-B inhibitors with a possible role in the treatment of neurodegenerative diseases such as Parkinson’s disease (PD).
A series of indole and benzofuran derivatives were synthesised and evaluated for their ability to inhibit monoamine oxidase (MAO) A and B.Figure optionsDownload as PowerPoint slide
Journal: European Journal of Medicinal Chemistry - Volume 45, Issue 10, October 2010, Pages 4458–4466