Synthesis, activity and pharmacokinetics of novel antibacterial 15-membered ring macrolones.
作者： Andrea Fajdetić , Adrijana Vinter , Hana Čipčić Paljetak , Jasna Padovan , Ivana Palej Jakopović
DOI: 10.1016/J.EJMECH.2011.05.002
关键词:
摘要: Abstract Synthesis, antibacterial activity and pharmacokinetic properties of a novel class macrolide antibiotics—macrolones—derived from azithromycin, comprising oxygen atom(s) in the linker either free or esterified quinolone 3-carboxylic group, are reported. Selected compounds showed excellent potency towards key erythromycin resistant respiratory pathogens. However, majority lacked good bioavailability. The isopropyl ester, compound 35, macrolone derivative with an elongated 29 best oral bioavailability rats, both accompanied overall microbiology profile addressing inducible constitutive MLSb as well efflux mediated resistance streptococci, while is more potent against staphylococci.
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