Investigating the Activity Spectrum for Ring-Substituted 8-Hydroxyquinolines

被引：44

作者：

Musiol, Robert ^{[1
]}

Jampilek, Josef ^{[2
,3
]}

Nycz, Jacek E. ^{[1
]}

Pesko, Matus ^{[4
]}

Carroll, James ^{[5
]}

Kralova, Katarina ^{[6
]}

Vejsova, Marcela ^{[7
]}

O'Mahony, Jim ^{[5
]}

Coffey, Aidan ^{[5
]}

Mrozek, Anna ^{[1
]}

Polanski, Jaroslaw ^{[1
]}

机构：

[1] Silesian Univ, Inst Chem, PL-40007 Katowice, Poland

[2] Zentiva KS, Prague, Czech Republic

[3] Univ Vet & Pharmaceut Sci, Fac Pharm, Dept Chem Drugs, Brno 61242, Czech Republic

[4] Comenius Univ, Fac Nat Sci, Dept Ecosozol & Physiotact, Bratislava 84215, Slovakia

[5] Cork Inst Technol, Dept Biol Sci, Cork, Ireland

[6] Comenius Univ, Fac Nat Sci, Inst Chem, Bratislava 84215, Slovakia

[7] Charles Univ Prague, Fac Pharm Hradec Kralove, Dept Biol & Med Sci, Hradec Kralove 50005, Czech Republic

来源：

MOLECULES | 2010年 / 15卷 / 01期

关键词：

quinolines; lipophilicity; PET inhibition; spinach chloroplasts; in vitro antifungal activity; in vitro antimycobacterial activity; PHOTOSYNTHETIC ELECTRON-TRANSPORT; POTENTIAL ANTILEUKOTRIENIC AGENTS; BIOLOGICAL-ACTIVITY SPECTRUM; SPINACH-CHLOROPLASTS; QUINOLINE ANALOGS; INHIBITION; ACID; DERIVATIVES; SERIES;

D O I：

10.3390/molecules15010288

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

In this study, a series of fourteen ring-substituted 8-hydroxyquinoline derivatives were prepared. The synthesis procedures are presented. The compounds were analyzed using RP-HPLC to determine lipophilicity. They were tested for their activity related to inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Primary in vitro screening of the synthesized compounds was also performed against four mycobacterial strains and against eight fungal strains. Several compounds showed biological activity comparable with or higher than the standards isoniazid or fluconazole. For all the compounds, the relationships between the lipophilicity and the chemical structure of the studied compounds are discussed.

引用

页码：288 / 304

页数：17

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