4″-O-(ω-Quinolylamino-alkylamino)propionyl derivatives of selected macrolides with the activity against the key erythromycin resistant respiratory pathogens

作者: A. Fajdetić , H. Čipčić Paljetak , G. Lazarevski , A. Hutinec , S. Alihodžić

DOI: 10.1016/J.BMC.2010.06.049

关键词: ChemistryMoietyLinkerTelithromycinKetolideQuinoloneAntibacterial activityClarithromycinAntibacterial agentStereochemistryOrganic chemistryClinical biochemistryMolecular medicineBiochemistryMolecular biologyDrug discoveryPharmaceutical Science

摘要: Abstract Four macrolides—6-O-methyl-8a-aza-8a-homoerythromycin, clarithromycin, azithromycin and 11,12-cyclic carbonate, have been selected for the construction of a series new quinolone derivatives. The moiety is connected to macrolide scaffold via diaminoaklyl 4″-O-propionyl ester chain varying length. At terminus linker attached one nitrogen atoms in at C(6) or C(7) quinolone. Many compounds described, particularly clarithromycin derivative 37, derivatives 48 55, exhibited excellent antibacterial activity against wide range clinically relevant macrolide-resistant organisms, with profiles superior that telithromycin, an enhanced spectrum ketolide.

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