Investigation of the Antimycobacterial Activity of 8-hydroxyquinolines

被引:12
作者
Cieslik, Wioleta [1 ]
Spaczynska, Ewelina [1 ]
Malarz, Katarzyna [1 ]
Tabak, Dominik [1 ]
Nevin, Eoghan [2 ]
O'Mahony, Jim [2 ]
Coffey, Aidan [2 ]
Mrozek-Wilczkiewicz, Anna [3 ,4 ]
Jampilek, Josef [5 ]
Musiol, Robert [1 ]
机构
[1] Univ Silesia, Inst Chem, Dept Organ Chem, Szkolna 9, PL-40007 Katowice, Poland
[2] Cork Inst Technol, Dept Biol Sci, Cork, Ireland
[3] Univ Silesia, A Chelkowski Inst Phys, PL-40007 Katowice, Poland
[4] Silesian Ctr Educ & Interdisciplinary Res, PL-41500 Chorzow, Poland
[5] Univ Vet & Pharmaceut Sci Brno, Fac Pharm, Dept Chem Drugs, Brno 61242, Czech Republic
关键词
Cytotoxicity; drug design; lipophilicity; mycobacterium; quinoline derivatives; styrylquinolines; BIOLOGICAL-ACTIVITY SPECTRUM; HERBICIDAL ACTIVITY; SPECTROSCOPIC CHARACTERIZATION; ANTIMICROBIAL ACTIVITY; DRUG DISCOVERY; DERIVATIVES; INHIBITORS; SERIES; SALICYLANILIDES; ANTIBACTERIAL;
D O I
10.2174/1573406410666150807111703
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of styrylquinolines and quinolineamides based on the 8-hydroxyquinoline moiety were investigated as potential antimycobacterial agents. The lipophilicity of the compounds was measured using RP-HPLC and the tests of their activity against Mycobacterium kansasii, the M. avium complex, M. smegmatis, M. abscessus, M. tuberculosis and M. avium paratuberculosis was performed. Several of the compounds that were obtained appeared to be more effective than isoniazid and ciprofloxacin. The 5,7-dinitro-8-hydroxyquinoline derivative possessed the highest potency against M. abscessus and M. Smegmatis, which was about twice as effective as ciprofloxacin, while 2-(2-hydroxystyryl)-8-hydroxyquinoline-7-carboxylic acid appeared to be comparable with the standard drugs that are against the M. avium complex. The structure activity relationships are discussed.
引用
收藏
页码:771 / 779
页数:9
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