Ring-substituted 4-hydroxy-1H-quinolin-2-ones: preparation and biological activity.
In the study, a series of twelve ring-substituted 4-hydroxy-1H-quinolin-2-one derivatives were prepared. The procedures for synthesis of the compounds are presented. The compounds were analyzed using RP-HPLC to determine lipophilicity and tested for their photosynthesis-inhibiting activity using spinach (Spinacia oleracea L.) chloroplasts. All the synthesized compounds were also evaluated for antifungal activity using in vitro screening with eight fungal strains. For all the compounds, the relationships between the lipophilicity and the chemical structure of the studied compounds are discussed, as well as their structure-activity relationships (SAR).
Jampilek
Josef
J
Zentiva ks, U Kabelovny 130, Prague 10, Czech Republic. josef.jampilek@zentiva.cz
Musiol
Robert
R
Pesko
Matus
M
Kralova
Katarina
K
Vejsova
Marcela
M
Carroll
James
J
Coffey
Aidan
A
Finster
Jacek
J
Tabak
Dominik
D
Niedbala
Halina
H
Kozik
Violetta
V
Polanski
Jaroslaw
J
Csollei
Jozef
J
Dohnal
Jiri
J
D000935:Antifungal Agents / Q000737:chemistry; D002736:Chloroplasts / Q000187:drug effects; D005658:Fungi / Q000187:drug effects; D057927:Hydrophobic and Hydrophilic Interactions; D006912:Hydroxyquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D010788:Photosynthesis / Q000187:drug effects; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D006912:Hydroxyquinolines; D015363:Quinolones