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

作　　者：YUAN Jing SU Xin ZHANG Xin CONG Lin GUO Chun 

机构地区：[1]Key Laboratory of Structure-based Drug Design ＆ Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China

出　　处：《Chemical Research in Chinese Universities》2011年第6期955-957,共3页高等学校化学研究（英文版）

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

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.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 in-hibitor Antifungal activity 

分 类 号：TQ463.53[化学工程—制药化工] TQ464.71