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

作     者：Vishnu Nayak Badavath Chandrani Nath Narayana Murthy Ganta Gulberk Ucar Barij Nayan Sinha Venkatesan Jayaprakash 

作者机构：Department of Pharmaceutical Sciences & Technology Birla Institute of Technology Department of Biochemistry Faculty of Pharmacy Hacettepe University 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2017年第28卷第7期

页      面：1528-1532页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 10[医学] 

基　　金：Birla Institute of Technology for providing financial support as a prestigious Institute fellowship 

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

摘      要：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.