Design, synthesis and antifungal activity of novel triazole derivatives with piperazine side chain
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摘要: 目的 基于唑类药物与靶酶相互作用模式,设计新型三唑类化合物,并测试其对常见致病真菌的抑制活性。 方法 采用酰化反应合成目标化合物,通过1H NMR和MS确证其化学结构,经微量液基稀释法测试体外抗真菌活性。 结果 合成了12个含C1甲基和哌嗪侧链的新型唑类化合物,它们均显示了中度至良好的抗真菌活性。 结论 部分目标化合物对白色念珠菌的活性优于对照药氟康唑,值得进一步深入构效关系研究。Abstract: Objective To design novel diazole derivatives on the basis of the binding mode of azole antifungal agents with the target enzyme and test their in vitro antifungal activities. Methods Acylation reaction of the oxidants was used to synthesize the target compounds, whose chemical structures were confirmed by 1H NMR and MS. Serial dilution method was used to determine the in vitro antifungal activities. Results Twelve novel azole compounds containing C1 methyl group and piperazine side chains were synthesized, which showed moderate to good antifungal activity. Conclusion Several target compounds showed better antifungal activity against Candida albicans than the positive drug fluconazole, which were worth to further investigating the structure-activity relationship.
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Key words:
- triazole /
- piperazine side chain /
- chemical synthesis /
- antifungal activities
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