Synthesis, activity and pharmacokinetics of novel antibacterial 15-membered ring macrolones (CROSBI ID 172190)
Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija
Podaci o odgovornosti
Fajdetić, Andreja ; Vinter, Adrijana ; Čipčić Paljetak, Hana ; Padovan, Jasna ; Palej Jakopović, Ivana ; Kapić, Samra ; Alihodžić, Sulejman ; Filić, Darko ; Modrić, Marina ; Košutić-Hulita, Nada ; Antolović, Roberto ; Ivezić Schoenfeld, Zrinka ; Mutak, Stjepan ; Eraković Haber, Vesna ; Spaventi, Radan
engleski
Synthesis, activity and pharmacokinetics of novel antibacterial 15-membered ring macrolones
Synthesis, antibacterial activity and pharmacokinetic properties of a novel class of macrolide antibioticsdmacrolonesdderived from azithromycin, comprising oxygen atom(s) in the linker and either free or esterified quinolone 3-carboxylic group, are reported. Selected compounds showed excellent antibacterial potency towards key erythromycin resistant respiratory pathogens. However, the majority of compounds lacked good bioavailability. The isopropyl ester, compound 35, and a macrolone derivative with an elongated linker 29 showed the best oral bioavailability in rats, both accompanied with an excellent overall microbiology profile addressing inducible and constitutive MLSb as well as efflux mediated macrolide resistance in streptococci, while compound 29 is more potent against staphylococci.
makrolide; resistance; antibacterial activity; pharmacokinetics; oral bioavailability
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Podaci o izdanju
46 (8)
2011.
3388-3397
objavljeno
0223-5234
10.1016/j.ejmech.2011.05.002
Povezanost rada
Kemija, Temeljne medicinske znanosti