Discovery of novel 2,3-dihydro-1H-inden-1-amine derivatives as selective monoamine oxidase B inhibitors |
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Authors: | Shiyu Li Xiao Lv Kai Cheng Yongbing Tian Xufeng Huang Haiyan Kong Yajun Duan Jihong Han Chenzhong Liao Zhouling Xie |
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Institution: | School of Food and Biological Engineering, Hefei University of Technology, Hefei, Anhui 230009, PR China |
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Abstract: | Inhibition of MAO-B has been an effective strategy for the treatment of Parkinson’s disease. To find more potent and selective MAO-B inhibitors with novel chemical scaffold, we designed and synthesized a series of new 2,3-dihydro-1H-inden-1-amine derivatives on basis of our previous study. Furthermore, the corresponding structure-activity relationship (SAR) of these compounds is detailedly discussed. Compounds L4 (IC50?=?0.11?μM), L8 (IC50?=?0.18?μM), L16 (IC50?=?0.27?μM) and L17 (IC50?=?0.48?μM) showed similar MAO-B inhibitory activity as Selegiline. Moreover, L4, L16 and L17 also exhibited comparable selectivity with Selegiline, indicating that L4, L16 and L17 could be promising selective MAO-B inhibitors for further study. |
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Keywords: | Monoamine oxidase B Selectivity 2 3-Dihydro-1H-inden-1-amine Structure activity relationship |
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