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

Autor: Stimac V; GSK Research Centre Zagreb Ltd, Zagreb, Croatia. vlado.z.stimac@gsk.com, Alihodzic S, Lazarevski G, Mutak S, Istuk ZM, Fajdetic A, Palej I, Paljetak HC, Marsic N, Padovan J, Tavcar B, Erakovic Haber V
Jazyk: angličtina
Zdroj: The Journal of antibiotics [J Antibiot (Tokyo)] 2009 Mar; Vol. 62 (3), pp. 133-44. Date of Electronic Publication: 2009 Feb 13.
DOI: 10.1038/ja.2009.1
Abstrakt: 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.
Databáze: MEDLINE