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• W2050781567 abstract "Aplysinopsins are tryptophan-derived natural products that have been isolated from a variety of marine organisms. Previous studies have shown aplysinopsin analogs to possess a variety of biological activities, including modulation of neurotransmissions. A series of fifty aplysinopsin analogs was synthesized and assayed for monoamine oxidase A and B inhibitory activity. Three compounds displayed significant MAO inhibitory activity and selectivity. The compound (E)-5-[(6-bromo-1H-indol-3-yl)methylene]-2-imino-1,3-dimethylimidazolidin-4-one (3x) possessed an IC50 of 5.6 nM at MAO-A and had a selectivity index of 80.24. An SAR study revealed that multiple N-methylations, one of which should be at position N-2′, and bromination at C-5 or C-6 are important factors for MAO-A potency and selectivity." @default.
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• W2050781567 date "2012-08-01" @default.
• W2050781567 modified "2023-10-18" @default.
• W2050781567 title "Synthesis and evaluation of aplysinopsin analogs as inhibitors of human monoamine oxidase A and B" @default.
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• W2050781567 doi "https://doi.org/10.1016/j.bmcl.2012.06.058" @default.
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