title: Ring-substituted 4-hydroxy-1H-quinolin-2-ones: preparation and biological activity.
abstract: 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).
authors.affiliation: Zentiva ks, U Kabelovny 130, Prague 10, Czech Republic. josef.jampilek@zentiva.cz
authors.forename: Josef
authors.initials: J
authors.lastname: Jampilek
authors.forename: Robert
authors.initials: R
authors.lastname: Musiol
authors.forename: Matus
authors.initials: M
authors.lastname: Pesko
authors.forename: Katarina
authors.initials: K
authors.lastname: Kralova
authors.forename: Marcela
authors.initials: M
authors.lastname: Vejsova
authors.forename: James
authors.initials: J
authors.lastname: Carroll
authors.forename: Aidan
authors.initials: A
authors.lastname: Coffey
authors.forename: Jacek
authors.initials: J
authors.lastname: Finster
authors.forename: Dominik
authors.initials: D
authors.lastname: Tabak
authors.forename: Halina
authors.initials: H
authors.lastname: Niedbala
authors.forename: Violetta
authors.initials: V
authors.lastname: Kozik
authors.forename: Jaroslaw
authors.initials: J
authors.lastname: Polanski
authors.forename: Jozef
authors.initials: J
authors.lastname: Csollei
authors.forename: Jiri
authors.initials: J
authors.lastname: Dohnal
mesh_terms: 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
chemical_list: D000935:Antifungal Agents; D006912:Hydroxyquinolines; D015363:Quinolones