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氟康唑类似物的研究进展

许克寒 黄蕾 吴俊琪 戚麟 金永生 俞世冲

许克寒, 黄蕾, 吴俊琪, 戚麟, 金永生, 俞世冲. 氟康唑类似物的研究进展[J]. 药学实践与服务, 2016, 34(2): 110-113,128. doi: 10.3969/j.issn.1006-0111.2016.02.004
引用本文: 许克寒, 黄蕾, 吴俊琪, 戚麟, 金永生, 俞世冲. 氟康唑类似物的研究进展[J]. 药学实践与服务, 2016, 34(2): 110-113,128. doi: 10.3969/j.issn.1006-0111.2016.02.004
XU Kehan, HUANG Lei, WU Junqi, QI Lin, JIN Yongsheng, YU Shichong. Research progress of fluconazole derivatives[J]. Journal of Pharmaceutical Practice and Service, 2016, 34(2): 110-113,128. doi: 10.3969/j.issn.1006-0111.2016.02.004
Citation: XU Kehan, HUANG Lei, WU Junqi, QI Lin, JIN Yongsheng, YU Shichong. Research progress of fluconazole derivatives[J]. Journal of Pharmaceutical Practice and Service, 2016, 34(2): 110-113,128. doi: 10.3969/j.issn.1006-0111.2016.02.004

氟康唑类似物的研究进展

doi: 10.3969/j.issn.1006-0111.2016.02.004
基金项目: 第二军医大学药学院药学实验中心孵化基地重点课题;本科学员创新实践能力孵化基地项目(2015YJ06)

Research progress of fluconazole derivatives

  • 摘要: 氟康唑是第三代三唑类抗真菌药物,具有水溶性好、广谱和低毒等优点,是临床上治疗真菌感染的首选药物。随着氟康唑耐药菌株的不断出现,研制新型氟康唑类似物成为重要的科研课题。通过对氟康唑结构的修饰,获得新型氟康唑类似物,为进一步的新药合成研究提供线索。
  • [1] Sobue S, Tan K, Haug-Pihale G. The effects of hepatic impairment on the pharmacokinetics of fosfluconazole and fluconazole following a single intravenous bolus injection of fosfluconazole[J]. Br J Clin Pharmacol, 2005,59(2):160-166.
    [2] Mora SJ, Cormick MP, Milanesio ME,et al. The photodynamic activity of a novel porphyrin derivative bearing a Fluconazole structure in different media and against Candida albicans[J]. Dyes Pigments, 2010, 87(3):234-240.
    [3] Zhou CH, Yu KG, Meng JP, et al. Dibenzimidazole and oniumcompound thereof, preparation method and medical use thereof:China, 101397276(A)[P].2009.
    [4] Francavilla C, Low E, Nair S, et al. Quaternary ammonium N,N-dichloroamines as topical antimicrobial agents[J]. Bioorg Med Chem Lett, 2009, 19(10):2731-2734.
    [5] Zhou CH, Mi JL, Wu J, et al. Triazole onium compound with antimicrobial activity, preparation method and medical use:China, 101391985(A)[P].2009.
    [6] Zhang YY, Mi JL, Zhou CH, et al. Synthesis of novel fluconazoliums and their evaluation for antibacterial and antifungal activities[J]. Eur J Med Chem, 2011, 46(9):4391-4402.
    [7] Sheng CQ, Zhang WN, Ji HT, et al. Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking[J]. J Med Chem, 2006, 49(8):2512-2525.
    [8] Chai XY, Zhang J, Yu S C, et al. Design,synthesis,and biological evaluation of novel 1-(1H-1,2,4-tri-Azole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols[J]. Bioorg Med Chem Lett, 2009, 19(6):1811-1814.
    [9] Wang WY, Sheng CQ, Che XY, et al. Design, synthesis, and antifungal activity of novel conformationally restricted triazole derivatives[J]. Arch Pharm(Weinheim), 2009, 342(12):732-739.
    [10] Li WH, Zhao L, Tan GG, et al. Enantioseparation of the new antifungal drug iodiconazole and structually related triaditimenol analogues by CE with neutral cyclodextrin additives[J]. Chromatograp-Hia, 2011, 73(8):1009-1014.
    [11] Yu S, Chai X, Hu N, et al. Synthesis and antifungal activity of the novel triazole compounds[J]. Medchemcomm, 2013, 4(4):704-708.
    [12] Yu S, Chai X, Hu H, et al. Synthesis and antifungal evaluation of the novel triazole derivatives as inhibitors of cytochrome P45014a-demethylase[J]. Eur J Med Chem, 2010, 45(3):4435-4445.
    [13] Chai XY, Zhang J, Yu SC, et al. Design,synthesis,and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols[J]. Bioorg Med Chem Lett, 2009, 19(6):1811-1814.
    [14] Giraud F, Loge C, Pagniez F, et al. Design, synthesis, and evaluation of 1-(N-benzylamino)-2-phn-yl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents[J]. Bioorg Med Chem Lett, 2008, 18(6):1820-1824.
    [15] Giraud F, Guillon R, Loge C, et al. Synthesis and structure-activity relationships of 2-phenyl-1-[(pyridinyl-and piperidinylmethyl)amino]-3-(1H-1,2,4-triazol-1-yl) propan-2-ols as antifungal agents[J]. Bioorg Med Chem Lett, 2009, 19(2):301-304.
    [16] Gan LL, Cai JL, Zhou CH. Advances in the research of piperazine compounds as receptor ligands[J]. Chin Pharma J, 2009, 44:1361-1368.
    [17] Gan LL, Lu YH, Zhou CH. Advances in the research of piperazine compounds as enzyme inhibitors[J]. Chin J Biochem Pharm, 2009, 30:127-131.
    [18] Cai JL, Lu YH, Gan LL, et al. Recent advance in the research of piperazine-containing compounds as antimicrobial agents[J]. Chin J Antibiot, 2009, 34:454-462.
    [19] Gan LL, Zhou CH. Synthesis of azole-containing piperazine derivatives and evaluation of their antibacterial, antifungal and cytotoxic activities[J].Bull Korean Chem Soc, 2010, 31(12):3684-3692.
    [20] Na YM. Synthesis and activity of novel 1-halogenobenzylindole linked triazole derivatives as antifungal agents[J]. Bull Korean Chem Soc, 2011, 32(1):307-310.
    [21] Zhao JX, Cao YY, Quan H, et al. In vitro and in vivo activities of HQQ-3, a new triazole antifungal agent[J]. Biol Pharm Bull, 2006, 29(10):2031-2034.
    [22] Xu JM, Cao YB, Zhang J, et al. Design, synthesis and antifungal activities of novel 1,2,4-triazole derivatives[J]. Eur J Med Chem, 2011, 46(7):3142-3148.
    [23] Jiang YW, Zhang J, Cao YB, et al. Synthesis, in vitro evaluation and molecular docking studies of new triazole derivatives as antifungal agents[J]. Bioorg Med Chem Lett, 2011, 21(15):4471-4475.
    [24] Tron GC, Pirali T, Billing RA, et al. Click chemistry reaction in medicinal chemistry:applications of the 1,3-dipolar cycloaddition between azides and alkynes[J].Med Res Rev, 2008, 28(2):278-308.
    [25] WeiJJ, Wang Y, Wang XL, et al. Recent advances of1,2,3-triazole compounds in medicinal chemistry[J]. Chin Pharm J, 2011, 46:481-485.
    [26] Wang BG, Yu SC, Chai XY, et al. Design synthesis and biological evaluation of 3-substituted triazole derivatives[J]. Chin Chem Lett, 2011, 22(5):519-522.
    [27] Fang B, Zhou CH, Rao XC. Synthesis and biological activities of novel amine-derived bis-azoles as potential antibacterial and antifungal agents[J]. Eur J Med Chem, 2010, 45(9):4388-4398.
    [28] Zhou CH, Fang B, Gan LL. Benzyl chloride tertiary amine double azole antimicrobial compounds, preparation and medical use thereof:China, 101323594(B)[P].2011.
    [29] Bendaha H, Yu L, Touzani R, et al. New azole antifungal agents with novel modes of action:synthesis and biological studies of new tridentate ligands based on pyrazole and triazole[J]. Eur J Med Chem, 2011, 46(9):4117-4124.
  • [1] 陈炳辰, 佟达丰, 万苗, 闫飞虎, 姚建忠.  UPLC-MS/MS法测定小鼠血浆中紫杉醇脂肪酸酯前药及其药代动力学研究 . 药学实践与服务, 2024, 42(): 1-5. doi: 10.12206/j.issn.2097-2024.202404082
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  • 收稿日期:  2015-01-04
  • 修回日期:  2015-04-24

氟康唑类似物的研究进展

doi: 10.3969/j.issn.1006-0111.2016.02.004
    基金项目:  第二军医大学药学院药学实验中心孵化基地重点课题;本科学员创新实践能力孵化基地项目(2015YJ06)

摘要: 氟康唑是第三代三唑类抗真菌药物,具有水溶性好、广谱和低毒等优点,是临床上治疗真菌感染的首选药物。随着氟康唑耐药菌株的不断出现,研制新型氟康唑类似物成为重要的科研课题。通过对氟康唑结构的修饰,获得新型氟康唑类似物,为进一步的新药合成研究提供线索。

English Abstract

许克寒, 黄蕾, 吴俊琪, 戚麟, 金永生, 俞世冲. 氟康唑类似物的研究进展[J]. 药学实践与服务, 2016, 34(2): 110-113,128. doi: 10.3969/j.issn.1006-0111.2016.02.004
引用本文: 许克寒, 黄蕾, 吴俊琪, 戚麟, 金永生, 俞世冲. 氟康唑类似物的研究进展[J]. 药学实践与服务, 2016, 34(2): 110-113,128. doi: 10.3969/j.issn.1006-0111.2016.02.004
XU Kehan, HUANG Lei, WU Junqi, QI Lin, JIN Yongsheng, YU Shichong. Research progress of fluconazole derivatives[J]. Journal of Pharmaceutical Practice and Service, 2016, 34(2): 110-113,128. doi: 10.3969/j.issn.1006-0111.2016.02.004
Citation: XU Kehan, HUANG Lei, WU Junqi, QI Lin, JIN Yongsheng, YU Shichong. Research progress of fluconazole derivatives[J]. Journal of Pharmaceutical Practice and Service, 2016, 34(2): 110-113,128. doi: 10.3969/j.issn.1006-0111.2016.02.004
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