6-Alkylquinolone-3-carboxylic acid tethered to macrolides synthesis and antimicrobial profile

Two series of clarithromycin and azithromycin derivatives with terminal 6-alkylquinolone-3-carboxylic unit with central ether bond in the linker were prepared and tested for antimicrobial activity. Quinolone-linker intermediates were prepared by Sonogashira-type C(6)-alkynylation of 6-iodo-quinolone...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2010-09, Vol.18 (17), p.6569-6577
Hauptverfasser:	Kapić, Samra, Čipčić Paljetak, Hana, Alihodžić, Sulejman, Antolović, Roberto, Eraković Haber, Vesna, Jarvest, Richard L., Holmes, David J., Broskey, John P., Hunt, Eric
Format:	Artikel
Sprache:	eng
Schlagworte:	6-(ω-Carboxy)-alkyl- N-ethyl-3-carboxylquinolones Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacology Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Antimicrobial activity Azithromycin - analogs & derivatives Azithromycin - chemistry Azithromycin - pharmacology Biological and medical sciences Clarithromycin - analogs & derivatives Clarithromycin - chemistry Clarithromycin - pharmacology Humans Macrolides - chemical synthesis Macrolides - chemistry Macrolides - pharmacology Medical sciences Microbial Sensitivity Tests Pharmacology. Drug treatments Quinolones - chemical synthesis Quinolones - chemistry Quinolones - pharmacology Structure-Activity Relationship Tethered macrolides
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