Ring-substituted 4-Hydroxy-1H-quinolin-2-ones: Preparation and Biological Activity ‡

Molecules

Josef Jampilek⁴  Robert Musiol¹  Matus Pesko⁵  Katarina Kralova⁵  Marcela Vejsova⁶  James Carroll²  Aidan Coffey²  Jacek Finster¹  Dominik Tabak¹  Halina Niedbala¹  Violetta Kozik¹  Jaroslaw Polanski¹  Jozef Csollei³ 

[1] Institute of Chemistry, University of Silesia, Szkolna 9, 40007 Katowice, Poland; E-mail:;Department of Biological Sciences, Cork Institute of Technology, Bishopstown, Cork, Ireland; E-mail:;Department of Chemical Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackeho 1/3, 61242 Brno, Czech Republic;Zentiva k.s., U kabelovny 130, 102 37 Prague 10, Czech Republic;Institute of Chemistry, Faculty of Natural Sciences, Comenius University, Mlynska dolina Ch-2, 84215 Bratislava, Slovakia; E-mail:;Department of Biological and Medical Sciences, Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic; E-mail:

关键词: Quinolinone derivatives;    Lipophilicity;    OER inhibition;    Spinach chloroplasts;    In vitro antifungal activity;    Structure-activity relationships.;   

DOI  :  10.3390/molecules14031145

来源: mdpi

【 摘 要 】

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).

【 授权许可】

CC BY   
© 2009 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland.