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首页> 外文期刊>Bioorganic and Medicinal Chemistry >Highly potent 3-pyrroline mechanism-based inhibitors of bovine plasma amine oxidase and mass spectrometric confirmation of cofactor derivatization
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Highly potent 3-pyrroline mechanism-based inhibitors of bovine plasma amine oxidase and mass spectrometric confirmation of cofactor derivatization

机译：牛血浆胺氧化酶的高效3-吡咯啉机理抑制剂和辅因子衍生化的质谱确认

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摘要

Despite the quinone-dependent copper amine oxidases being described as having the ability to metabolize unbranched primary amines to the corresponding aldehydes, we previously showed that the secondary amines 3-pyrrolines are metabolized as mechanism-based inactivators of bovine plasma amine oxidase (BPAO), and that the 3-(3-nitro-4-methoxyphenyl)-substituted analog was a particularly potent and efficient inactivator. We now show that additional 3-aryl-3-pyrrolines containing highly electron-withdrawing aryl groups (pyridyl, quinolyl, isoquinolyl, and pentafluorophenyl) are some of the most potent inactivators of BPAO reported to date. We also provide mass spectroscopic confirmation of the proposed mechanism of inhibition involving pyrrolyla-tion of the active-site cofactor, through identification by MALDI-TOF and LC-ESI-MS/MS of the (3-arylpyrrol-l-yl)resorcinol derivatives of the cofactor-containing thermolytic peptides.
机译：尽管描述了依赖醌的铜胺氧化酶具有将直链伯胺代谢为相应醛的能力，但我们先前显示仲胺3-吡咯啉被代谢为牛血浆胺氧化酶（BPAO）的基于机理的灭活剂，并且3-（3-硝基-4-甲氧基苯基）-取代的类似物是特别有效的灭活剂。我们现在表明，含有高度吸电子芳基（吡啶基，喹啉基，异喹啉基和五氟苯基）的其他3-芳基-3-吡咯啉是迄今为止报道的BPAO最有效的灭活剂。我们还通过MALDI-TOF和LC-ESI-MS / MS鉴定了（3-芳基吡咯-1-基）间苯二酚衍生物，通过质谱方法证实了涉及活性位点辅因子热解的拟议抑制机理含辅因子的热解肽。

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