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首页> 外文期刊>Chemical and Pharmaceutical Bulletin >Design, Synthesis, Antifungal Activity and Molecular Docking of Thiochroman-4-one Derivatives
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Design, Synthesis, Antifungal Activity and Molecular Docking of Thiochroman-4-one Derivatives

机译：硫代锡-4-一种衍生物的设计，合成，抗真菌活性和分子对接

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摘要

N-Myristoyltransferase (NMT) has been validated pre-clinically as a target for treatment of fungal infections. Various substituted thiochroman-4-one derivatives have been synthesized by an efficient method. The synthesized compounds 7a-y and 8a-t were evaluated for their in vitro antifungal activity against the Canidia albicans, Cryptococcus neoformans, Epidermophyton floccosum, Mucor racemosus, Microsporum gypseum and Aspergillus nigerstrain. A series of compounds exhibited significant activity (minimal inhibitory concentrotion (MIC)=0.5-16 mu g/mL) against Canidia albicans and Cryptococcus neoformans. The antifungal activity of compound 7b was reached to that of fluconazole, which can serve as a good starting point for further studies of structural diversity of the NMT inhibitors. The molecular docking studies revealed an interesting binding profile with very high receptor affinity for NMT of Canidia albicans.
机译：N-Myristoyltransferase（NMT）已在临床上被验证为治疗真菌感染的靶标。 通过有效的方法合成了各种取代的硫醇-4-一种衍生物。 评价合成化合物7a-y和8a-t，用于针对Canidia醛糖醛植物，嗜碱性蛋白酶，ePiDermophyton floccosum，粘膜术，微孢子孢菌和曲霉菌菌株的体外抗真菌活性。 一系列化合物具有显着的活性（最小抑制浓度（MIC）=0.5-16μg/ ml），对Canidia醛糖苷和碱性细胞新族商。 将化合物7B的抗真菌活性达到氟康唑的抗真菌活性，其可以作为进一步研究NMT抑制剂的结构多样性的良好起点。 分子对接研究揭示了一种有趣的结合曲线，具有非常高的Canidia醛肽的NMT受体亲和力。

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  • 作者

    Zhong Yifan; Han Xiaoyan; Li Shengbin; Qi Hui; Song Yali; Qiao Xiaoqiang;

  • 作者单位

    Hebei Univ Coll Pharmaceut Sci Key Lab Pharmaceut Qual Control Hebei Prov Baoding 071002 Hebei Peoples R China;

    Hebei Univ Coll Pharmaceut Sci Key Lab Pharmaceut Qual Control Hebei Prov Baoding 071002 Hebei Peoples R China;

    Hebei Univ Coll Pharmaceut Sci Key Lab Pharmaceut Qual Control Hebei Prov Baoding 071002 Hebei Peoples R China;

    Hebei Univ Coll Pharmaceut Sci Key Lab Pharmaceut Qual Control Hebei Prov Baoding 071002 Hebei Peoples R China;

    Hebei Univ Coll Pharmaceut Sci Key Lab Pharmaceut Qual Control Hebei Prov Baoding 071002 Hebei Peoples R China;

    Hebei Univ Coll Pharmaceut Sci Key Lab Pharmaceut Qual Control Hebei Prov Baoding 071002 Hebei Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药学;化学;
  • 关键词

    thiochroman-4-one; antifungal; molecular docking; N-myristoyltransferase; inhibitor;

    机译：硫核糖-4-一;抗真菌;分子对接;n-myristoyltransferase;抑制剂;

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