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Design, Synthesis and Antifungal Activity of 6-Fluoro-3,3a,4,5-tetrahydro-2H-pyrazolo[4,3-c]-quinoline-2-carboxamide Derivatives
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作者 YUAN Jing SU Xin ZHANG Xin CONG Lin GUO Chun 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2011年第6期955-957,共3页
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 fr... 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. 展开更多
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
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Synthesis and Crystal Structure of Ethyl 2-(6-(1,3-Dioxo-4,5,6,7-tetrahydro-1H-isoindol-2(3H)-yl)-7-fluoro-3-oxo-2H-benzo[b][1,4]oxazin-4(3H)-yl) Butanoate
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作者 吴道新 罗斐贤 +4 位作者 莫洪波 王晓光 任叶果 SIMPSON Jim 黄明智 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2009年第5期585-589,共5页
The title compound ethyl 2-(6-(1,3-dioxo-4,5,6,7-tetrahydro-lH-isoindol-2(3H)- yl)-7-fluoro-3-oxo-2H-benzo[b][1,4]oxazin-4(3H)-yl) butanoate 3 was synthesized by the reaction of ethyl 2-(6-amino-7-fluoro-3-ox... The title compound ethyl 2-(6-(1,3-dioxo-4,5,6,7-tetrahydro-lH-isoindol-2(3H)- yl)-7-fluoro-3-oxo-2H-benzo[b][1,4]oxazin-4(3H)-yl) butanoate 3 was synthesized by the reaction of ethyl 2-(6-amino-7-fluoro-3-oxo-2H-benzo[b][1,4]oxazin-4(3H)-yl) butanoate with 4,5,6,7- tetraydrophthalic anhydride, and its structure was determined by X-ray single-crystal diffraction. The crystal belongs to the monoclinic system, space group P2 1/n with a = 9.3469(2), b = 16.7715(5), c = 13.7153(4) A, β= 104.9680(10)°, μ = 0.107 mm^-1, Mr = 430.42, V= 2077.08(10) ,A3, Z= 4, Dc = 1.376 g/cm3, F(000) = 904, T= 296(2) K, R = 0.0508 and wR = 0.1478. 展开更多
关键词 synthesis crystal structure ethyl 2-(6-amino-7-fluoro-3-oxo-2H-benzo[b][1 4]oxazin-43H)-yl) butanoate herbicidal protox inhibitors
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STUDIES ON THE SYNTHESIS OF D-GLUCURONIC ACID DERIVATIVES OF 2-BUTOXY-5-FLUORO-3H-4-PYRIMIDONE AND THEIR ANTICANCER ACTIVITIES
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作者 Chang Jun SUN Zai Cheng CHEN Yi Gui WANG Peng XUE Department of Chemistry,Shandong University,Jinan,250100Feng Yao LIU Department of Chemistry,Zaozhuang Teachers College,Zaozhuang,Shandong,277000 《Chinese Chemical Letters》 SCIE CAS CSCD 1993年第3期197-198,共2页
2-Butoxy-5-fluoro-3H-4-pyrimidone derivatives of D-glucuronic acid having 0-glycosidic linkage or N-glycosidic linkage were synthesized and their anticancer activity tested.Their structures were confirmed by elementar... 2-Butoxy-5-fluoro-3H-4-pyrimidone derivatives of D-glucuronic acid having 0-glycosidic linkage or N-glycosidic linkage were synthesized and their anticancer activity tested.Their structures were confirmed by elementary analysis,IR spectra and ~1HNMR. 展开更多
关键词 STUDIES ON THE SYNTHESIS OF D-GLUCURONIC ACID DERIVATIVES OF 2-BUTOXY-5-fluoro-3H-4-PYRIMIDONE AND THEIR ANTICANCER ACTIVITIES ACID
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一种新的柱前衍生RP-HPLC法分析酱腌菜中的生物胺 被引量:7
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作者 郭晓丽 李二虎 +6 位作者 王鲁峰 刘齐 李芯郁 余佳 钟武 宋雅东 潘思轶 《现代食品科技》 EI CAS 北大核心 2017年第10期237-244,共8页
以4-fluoro-3-nitrobenzo-trifluoride(FNBT)为衍生剂,N,N-diisopropylethyl-amine(DIPEA)为催化剂,建立了一种新的柱前衍生-反高效液相色谱检测法(RP-HPLC)同时测定酱腌菜中的8种生物胺(组胺、色胺、β-苯乙胺、腐胺、酪胺、尸胺、亚... 以4-fluoro-3-nitrobenzo-trifluoride(FNBT)为衍生剂,N,N-diisopropylethyl-amine(DIPEA)为催化剂,建立了一种新的柱前衍生-反高效液相色谱检测法(RP-HPLC)同时测定酱腌菜中的8种生物胺(组胺、色胺、β-苯乙胺、腐胺、酪胺、尸胺、亚精胺及精胺)。采用硼酸盐缓冲溶液为衍生介质,在60℃下衍生反应30 min,使用C18色谱柱分离,以乙腈和超纯水为流动相梯度洗脱,流速1.00m L/min,紫外检测波长242 nm。在0.5~100 mg/L浓度范围内,8种生物胺呈现良好的线性相关(r2≥0.999),方法的检出限(LODs)为0.013~0.053 mg/L,定量限(LOQs)为0.044~0.176 mg/L,加标平均回收率为93.47%~99.87%,相对标准偏差(RSD)为0.47%~3.67%。采用该方法对26种市售酱腌菜中的生物胺进行了分析,发酵型酱腌菜中的生物胺总量范围为40.57~692.82 mg/kg,非发酵型酱腌菜中的生物胺总量范围为9.86~270.93 mg/kg。发酵型酱腌菜中8种生物胺单体的平均含量均高于非发酵型酱腌菜。该方法简单、准确和可靠,可适用于酱腌菜中生物胺的快速分析。 展开更多
关键词 4-fluoro-3-nitrobenzo-trifluoride(FNBT) 反相高效液相色谱(RP-HPLC) 生物胺 酱腌菜
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