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Synthesis and biological activity of 4″-O-acyl derivatives of 14- and 15-membered macrolides linked to ω-quinolone-carboxylic unit

2010; Elsevier BV; Volume: 18; Issue: 17 Linguagem: Inglês

10.1016/j.bmc.2010.06.050

1464-3391

Maja Matanović Škugor, Vlado Štimac, Ivana Palej, Đurdjica Lugarić, Hana Čipčić Paljetak, Darko Filić, Marina Modrić, Ivica Đilović, Dubravka Gembarovski, Stjepan Mutak, Vesna Eraković, David Holmes, Zrinka Ivezic‐Schoenfeld, Sulejman Alihodžić,

Synthesis and Biological Evaluation

The synthesis and antimicrobial activity of a new class of macrolide antibiotics which consist of a macrolide scaffold and a quinolone unit covalently connected by an appropriate linker are described. Optimization of several synthetic steps and structural properties of lead compound 26 are discussed. Promising antibacterial properties of this compound and some of its analogues are reported.