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Design, synthesis and MAO inhibitory activity of 2-(arylmethylidene)-2,3-dihydro-1-benzofuran-3-one derivatives

Chinese Chemical Letters 2017年第7期28卷 1528-1532页

作者： Vishnu Nayak Badavath Chandrani Nath Narayana Murthy Ganta Gulberk Ucar Barij Nayan Sinha venkatesan jayaprakash Department of Pharmaceutical Sciences & Technology Birla Institute of Technology Department of Biochemistry Faculty of Pharmacy Hacettepe University

A series of 2-（arylmethylidene）-2,3-dihydro-1-benzofuran-3-one derivatives（aurones, 1–20） were synthesized and screened for their inhibitory activity against h MAO. Seventeen compounds（1–5, 7–17,19） were found to be selective towards h MAO-B, while two were non-selective（6 and 20） and one（18）selective towards h MAO-A. Compound 17（Ki = 0.10 0.01 mmol/L） was found to be equally potent and selective towards h MAO-B, when compared with the standard drug Selegiline（Ki = 0.12 0.01 mmol/L）.Nature and position of substitution in aryl ring at 2nd position of benzofuranone influences h MAO-B inhibitory potency, while their structural bulkiness influences selectivity between h MAO-A and h *** docking simulation was also carried out to understand the interaction of inhibitor with the enzyme at molecular level, and we found the docking results were in good agreement with the experimental values. Comparison of the activity profile of the aurones with their corresponding flavones reported earlier by our group revealed that there exists no difference in potency as well as selectivity.

关键词： 2-(Arylmethylidene)-2 3-dihydro-1-benzofuran-3-one derivatives hMAO inhibitors Molecular docking simulation Synthesis

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