Design, Synthesis and Antifungal Activity of 6-Fluoro-3, 3a, 4, 5-tetrahydro-2H-pyrazolo [4, 3-c]-quinoline-2-carboxamide Derivatives
查看参考文献20篇
文摘
|
A series of 6-fluoro-3, 3a, 4, 5-tetrahydro-2H-pyrazolo[4, 3-c]quinoline-2-carboxanide 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 'H 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. |
来源
|
Chemical Research in Chinese Universities
,2011,27(6):955-957 【核心库】
|
关键词
|
6-Fluoro-3, 3a, 4, 5-tetrahydro-2H-pyrazolo[4, 3-c]quinoline-2-carboxamide derivative
;
Cysteine protease inhibitor
;
Antifungal activity Article ID 1005-9040(2011)-06-955-03
|
地址
|
Shenyang Pharmaceutical University, Key Laboratory of Structure-based Drug Design & Discovery, Ministry of Education, Shenyang, 110016
|
语种
|
英文 |
文献类型
|
研究性论文 |
ISSN
|
1005-9040 |
学科
|
化学 |
基金
|
Supported by the National Science and Technology Major Projects of China
|
文献收藏号
|
CSCD:4377190
|
参考文献 共
20
共1页
|
1.
Decory T R.
Eur. J. Med. Chem,1989,24:563
|
CSCD被引
1
次
|
|
|
|
2.
Lamb D C.
Pestic Sci,1996,46:294
|
CSCD被引
1
次
|
|
|
|
3.
Haller M A.
Antimicrob. Agents Chemother,1994,43:169
|
CSCD被引
1
次
|
|
|
|
4.
Elizabeth A S.
Clin. Ther,2002,24:351
|
CSCD被引
17
次
|
|
|
|
5.
Ji H.
J. Med. Chem,2003,46:47
|
CSCD被引
1
次
|
|
|
|
6.
Frank C O.
Trends in Microbiology,2003,11:272
|
CSCD被引
2
次
|
|
|
|
7.
Wan J. Synthesis, Structure and Biological Activities of 2-(1H- 1,2,3-Benzotriazol-1 -yl )-1-( 4- methylphenyl )-2-(1H-1,2,4-triazol-l-yl)-1-ethanone.
Chem. Res. Chinese Universities,2006,22(4):465
|
CSCD被引
2
次
|
|
|
|
8.
Xu L Z. Syntheses and Biological Activities of Novel Benzotriazole Compounds Containing a Thioamide Group.
Chem. Res. Chinese Universities,2006,22(5):574
|
CSCD被引
1
次
|
|
|
|
9.
Kiran S.
Synth. React. Inorg. Met. Org. Chem,1987,3:385
|
CSCD被引
1
次
|
|
|
|
10.
Margolin N.
Biol. Chem,1997,272:7223
|
CSCD被引
1
次
|
|
|
|
11.
Thornberry N A.
Biol. Chem,1997,272:17901
|
CSCD被引
1
次
|
|
|
|
12.
Liu Y.
Drug Discov. Ther,2008,2:216
|
CSCD被引
1
次
|
|
|
|
13.
Qi P.
Chin. J. Chem,2003,13:134
|
CSCD被引
1
次
|
|
|
|
14.
Alex C.
Biol & Med. Chem,2007,15:273
|
CSCD被引
1
次
|
|
|
|
15.
Tan C X.
Chin J. Org. Chem,2008,28:1836
|
CSCD被引
1
次
|
|
|
|
16.
Ferrarini P L.
Eur. J. Med. Chem,2000,35:815
|
CSCD被引
4
次
|
|
|
|
17.
Zhu Q H.
Chin. J. Med. Chem,2000,10:5
|
CSCD被引
1
次
|
|
|
|
18.
Huo N.
Organic Chemistry,1981:499
|
CSCD被引
1
次
|
|
|
|
19.
Chen H T.
Acta Pharmaceutica Sinica,1991,26:183
|
CSCD被引
4
次
|
|
|
|
20.
Gao F.
Chin. J. Applied Chem,2004,21:374
|
CSCD被引
1
次
|
|
|
|
|