Investigating the activity spectrum for ring-substituted 8-hydroxyquinolines.
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.
Musiol
Robert
R
Institute of Chemistry, University of Silesia, Szkolna 9, 40007 Katowice, Poland. robert.musiol@us.edu.pl
Jampilek
Josef
J
Nycz
Jacek E
JE
Pesko
Matus
M
Carroll
James
J
Kralova
Katarina
K
Vejsova
Marcela
M
O'Mahony
Jim
J
Coffey
Aidan
A
Mrozek
Anna
A
Polanski
Jaroslaw
J
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002176:Candida albicans / Q000187:drug effects; D002736:Chloroplasts / Q000187:drug effects / Q000378:metabolism; D004579:Electron Transport / Q000187:drug effects; D006912:Hydroxyquinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D009161:Mycobacterium / Q000187:drug effects; D010788:Photosynthesis / Q000187:drug effects; D018724:Spinacia oleracea / Q000187:drug effects / Q000378:metabolism
D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D006912:Hydroxyquinolines