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Bioorg Med Chem Lett. 2019 May 1;29(9):1090-1093. doi: 10.1016/j.bmcl.2019.02.030. Epub 2019 Feb 27.

Discovery of novel 2,3-dihydro-1H-inden-1-amine derivatives as selective monoamine oxidase B inhibitors.

Author information

1
School of Food and Biological Engineering, Hefei University of Technology, Hefei, Anhui 230009, PR China.
2
School of Food and Biological Engineering, Hefei University of Technology, Hefei, Anhui 230009, PR China. Electronic address: czliao@hfut.edu.cn.
3
School of Food and Biological Engineering, Hefei University of Technology, Hefei, Anhui 230009, PR China. Electronic address: zhoulingxie@hfut.edu.cn.

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.

KEYWORDS:

2,3-Dihydro-1H-inden-1-amine; Monoamine oxidase B; Selectivity; Structure activity relationship

PMID:
30833108
DOI:
10.1016/j.bmcl.2019.02.030

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