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Synthesis and biological evaluation of 1,2,4,5-tetrasubstituted imidazoles

机译:1,2,5-四氢咪唑的合成与生物学评价

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摘要

Tetrasubstituted imidazoles were synthesized in high yields via the four-component reaction of aromatic aldehydes, amines, substituted benzils and ammonium acetate catalyzed by a porous CeO2 nanorod. Their anti-cancer activities on the Huh-7 hepatocellular carcinoma cell and antibacterial activities on four bacterial species (wild-type Escherichia coli, wild-type Staphylococcus aureus, Pseudomonas aeruginosa PAM1032 and Escherichia coli-NMD-1) in vitro were evaluated. One compound (5p) was screened out because of its high inhibition rate on all four bacterials at 100 mu g/mL. Three products (5p, 5t and 5y) showed a high inhibition rate on the Huh-7 hepatocellular carcinoma cell at 10 mu g/mL. The results indicated their potential in new drug development.
机译:通过由多孔CeO2纳米棒催化的芳香醛,胺,取代的苯并和乙酸铵的四组分反应以高产率合成四氢吡嗪。 评估其对肝细胞癌细胞和四种细菌种类的抗菌活性的抗癌活动(野生型大肠杆菌,野生型葡萄球菌,假鼠铜绿假单胞菌PAM1032和大肠杆菌Coli-NMD-1)。 筛选一种化合物(5p),因为其在100μg/ ml的所有四种细菌上的高抑制率高。 三种产品(5P,5T和5Y)在Huh-7肝细胞癌细胞上显示出高抑制率为10μg/ mL。 结果表明了它们在新药开发中的潜力。

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  • 作者单位

    Jiangsu Normal Univ Sch Chem &

    Chem Engn Xuzhou 221116 Peoples R China;

    Jiangsu Normal Univ Sch Chem &

    Chem Engn Xuzhou 221116 Peoples R China;

    Jiangsu Normal Univ Sch Chem &

    Chem Engn Xuzhou 221116 Peoples R China;

    Jiangsu Normal Univ Sch Chem &

    Chem Engn Xuzhou 221116 Peoples R China;

    Jiangsu Normal Univ Sch Chem &

    Chem Engn Xuzhou 221116 Peoples R China;

    Jiangsu Normal Univ Sch Chem &

    Chem Engn Xuzhou 221116 Peoples R China;

    Jiangsu Normal Univ Sch Chem &

    Chem Engn Xuzhou 221116 Peoples R China;

    Jiangsu Normal Univ State Key Lab Cultivat Construct Base Biotechnol Xuzhou 221116 Peoples R China;

    Jiangsu Normal Univ State Key Lab Cultivat Construct Base Biotechnol Xuzhou 221116 Peoples R China;

    Jiangsu Normal Univ Sch Chem &

    Chem Engn Xuzhou 221116 Peoples R China;

    Jiangsu Normal Univ State Key Lab Cultivat Construct Base Biotechnol Xuzhou 221116 Peoples R China;

    Jiangsu Normal Univ State Key Lab Cultivat Construct Base Biotechnol Xuzhou 221116 Peoples R China;

    Jiangsu Normal Univ Sch Chem &

    Chem Engn Xuzhou 221116 Peoples R China;

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

    Tetrasubstituted imidazoles; Porous CeO2 Nanorod; Synthesis; Bioactivity;

    机译:四氢咪唑;多孔CEO2纳米棒;合成;生物活性;

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