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首页> 外文期刊>ACS medicinal chemistry letters >Highly Efficient Synthesis of 1,3-Dihydroxy-2-carboxycarbazole and Its Neuroprotective Effects
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Highly Efficient Synthesis of 1,3-Dihydroxy-2-carboxycarbazole and Its Neuroprotective Effects

机译:1,3-二羟基-2-羧基咔唑的高效合成及其神经保护作用

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摘要

Carbazoles represent a family of tricyclic compounds that widely appeared in nature. Numerous studies have revealed a diverse array of bioactivity associated with this scaffold. In the present study, a novel and highly efficient methodology for preparing 1,3-dihydroxy-2-carboxycarbazole from indole-3-acetic acid and Meldrum's acid was developed. Furthermore, biological characterization demonstrated that this multisubstituted carbazole analogue exhibited inhibitory activity on A beta aggregation, antioxidative properties, and promising neuroprotective activities in a cellular model of Alzheimer's disease, thus further supporting the valuable application of this synthetic methodology in search for effective neuroprotectants.
机译:咔唑代表自然界中广泛出现的三环化合物家族。大量研究揭示了与此支架相关的多种生物活性。在本研究中,开发了一种新颖且高效的方法,由吲哚-3-乙酸和Meldrum酸制备1,3-二羟基-2-羧基咔唑。此外,生物学表征表明,该多取代咔唑类似物在阿尔茨海默氏病细胞模型中表现出对Aβ聚集的抑制活性,抗氧化特性和有希望的神经保护活性,从而进一步支持了这种合成方法在寻找有效神经保护剂中的宝贵应用。

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