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高等学校化学研究 ›› 2011, Vol. 27 ›› Issue (6): 955-957.

• Articles • 上一篇    下一篇

Design, Synthesis and Antifungal Activity of 6-Fluoro-3,3a,4,5-tetrahydro-2H-pyrazolo[4,3-c]-quinoline-2-carboxamide Derivatives

YUAN Jing, SU Xin, ZHANG Xin, CONG Lin and GUO Chun*   

  1. Key Laboratory of Structure-based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China
  • 收稿日期:2011-01-13 修回日期:2011-04-25 出版日期:2011-11-25 发布日期:2011-11-07
  • 通讯作者: GUO Chun E-mail:chunguo63@yahoo.com.cn
  • 基金资助:

    Supported by the National Science and Technology Major Projects of China(No.2009ZX09301-012).

Design, Synthesis and Antifungal Activity of 6-fluoro-3,3a,4,5-tetrahydro-2H-pyrazolo[4,3-c]quinoline-2-carboxamide Derivatives

YUAN Jing, SU Xin, ZHANG Xin, CONG Lin and GUO Chun*   

  1. Key Laboratory of Structure-based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China
  • Received:2011-01-13 Revised:2011-04-25 Online:2011-11-25 Published:2011-11-07
  • Contact: GUO Chun E-mail:chunguo63@yahoo.com.cn
  • Supported by:

    Supported by the National Science and Technology Major Projects of China(No.2009ZX09301-012).

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摘要： A series of 6-fluoro-3,3a,4,5-tetrahydro-2H-pyrazolo[4,3-c]quinoline-2-carboxamide derivatives was designed based on the bioisosterism and combination principle in drug design. The target compounds were synthesized from substituted aniline through Michael addition, cyclization, Mannich reaction and condensation with 4-substituted semicarbazides, and the structures were confirmed by mass spectrometry(MS) and 1H NMR. The antifungal assay was carried out in vitro by two-fold dilution. The result shows that all the compounds are of antifungal activities against the tested fungi at different levels.

关键词: 6-Fluoro-3,3a,4,5-tetrahydro-2H-pyrazolo[4,3-c]quinoline-2-carboxamide derivative, Cysteine protease inhibitor, Antifungal activity

Abstract: A series of 6-fluoro-3,3a,4,5-tetrahydro-2H-pyrazolo[4,3-c]quinoline-2-carboxamide derivatives was designed based on the bioisosterism and combination principle in drug design. The target compounds were synthesized from substituted aniline through Michael addition, cyclization, Mannich reaction and condensation with 4-substituted semicarbazides, and the structures were confirmed by mass spectrometry(MS) and 1H NMR. The antifungal assay was carried out in vitro by two-fold dilution. The result shows that all the compounds are of antifungal activities against the tested fungi at different levels.

Key words: 6-Fluoro-3,3a,4,5-tetrahydro-2H-pyrazolo[4,3-c]quinoline-2-carboxamide derivative, Cysteine protease inhibitor, Antifungal activity