Popis: |
The bark of the Cinchona trees is the source of a variety of alkaloids, the most famous being cinchonine, cinchonidine, quinine and quinidine. They are useful in organic chemistry as organocatalysts in stereoselective syntheses, but also in medicine, since they possess various analgesics, anti-inflammatory and anti–arrhythmic properties. To investigate a new class of antimicrobials that could direct to the discovery of a novel scaffold, a series of quaternary derivatives of cinchonines and their corresponding pseudo-enantiomeric cinchonidines were synthesized. All compounds were prepared in good yields and characterized by standard analytical spectroscopy methods. The antibacterial activities of all compounds were evaluated against seven recent clinical isolates of antibiotic susceptible Gram- positive and resistant Gram-negative pathogens. The bioactive assays, antibacterial efficiency, cytotoxicity and classification model build by principal component analysis for all compounds will be discussed. Supported by Croatian Science Foundation, Project No 3775 ADESIRE |