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首页> 外文期刊>Russian Chemical Bulletin >Influence of the gamma-carboline and carbazole pharmacophore moieties on anticholinesterase and antiradical activity of multifunctional agents for the treatment of neurodegenerative diseases
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Influence of the gamma-carboline and carbazole pharmacophore moieties on anticholinesterase and antiradical activity of multifunctional agents for the treatment of neurodegenerative diseases

机译：γ-咔唑和咔唑药物部分对多官能药物治疗神经变性疾病抗胆碱酯酶及抗胆碱活性的影响

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摘要

A comparative analysis of the esterase profile and antiradical activity of two groups of hybrid compounds, viz., tetrahydro-gamma-carboline conjugates with carbazoles and tetrahydrocarbazoles (I) and carbazole conjugates with carbazoles and tetrahydrocarbazoles (II), was performed. The replacement of the tetrahydro-gamma-carboline moiety (conjugates I) by the carbazole group (conjugates II) was shown to significantly reduce the ability of the compounds to inhibit butyrylcholinesterase (BChE) and scavenge free radicals. The tetrahydro-gamma-carboline-tetrahydrocarbazole combination is optimal in terms of both high anti-BChE activity and free radical scavenging ability. According to molecular modeling calculations, the stronger binding of tetrahydro-gamma-carboline conjugates (I) in the BChE active site compared to carbazole conjugates (II) is attributed to the ability of I to form ionic and pi-cation interactions with amino acid residues lining the BChE gorge. Therefore, conjugates of tetrahydro-gamma-carboline and tetrahydrocarbazole derivatives are the most promising compounds for the design of new multitarget drugs combining cognitive-stimulating and antioxidant properties.
机译：进行两组杂化化合物，杂交化合物，γ-咔唑（I）与咔唑和四氢咔唑（II）的四氢-γ-咔唑（I）和咔唑缀合物的比较分析。显示通过咔唑基团（缀合物II）替换四氢γ-胶质碱部分（缀合物I），显着降低化合物抑制丁酰胆碱酯酶（BCHE）和清除自由基的能力。在高抗BCHE活性和自由基清除能力方面，四氢γ-胶原酚 - 四氢咔唑组合是最佳的。根据分子建模计算，与咔唑缀合物（II）相比，BCHE活性位点中的四氢-γ-咔啉缀合物（I）的较强结合归因于i与氨基酸残基形成离子和Pi-阳离子相互作用的能力衬氏峡谷。因此，四氢 - γ-碱和四氢咔唑衍生物的缀合物是最有前途的化合物，用于设计具有认知刺激和抗氧化特性的新型多元药物。

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