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Synthesis and biological properties of 4″-O-acyl derivatives of 8a-Aza-8a-homoerythromycin

2009; Springer Nature; Volume: 62; Issue: 3 Linguagem: Inglês

10.1038/ja.2009.1

1881-1469

Vlado Štimac, Sulejman Alihodžić, Gorjana Lazarevski, Stjepan Mutak, Zorica Marušić Ištuk, Andrea Fajdetić, Ivana Palej, Hana Čipčić Paljetak, Jasna Padovan, Branka Tavčar, Vesna Eraković,

Antimicrobial Resistance in Staphylococcus

A series of 4''-O-acyl derivatives of 8a-aza-8a-homoerythromycins A were synthesized and tested against Gram-positive and Gram-negative bacteria. Derivatives of 8a-aza-8a-homoerythromycin A have potent anti-bacterial activity against not only azithromycin-susceptible strains, but also efflux (M) and inducible macrolide-lincosamide-streptogramin-resistant Gram-positive pathogens. These compounds show moderate to high clearance and low oral bioavailability in preliminary in vivo pharmacokinetic studies in rat.