engleski

Synthesis and Biological Properties of 4''-O-Acyl Derivatives of 8a-Aza-8a-homoerythromycin

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

azalide; acylide; antibacterial activity; pharmacokinetics; structure-activity relationship

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