- Synthesis and antibacterial evaluation of novel 4′-glycyl linked quinolyl-azithromycins with potent activity against macrolide-resistant pathogens
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A new azithromycin-based series of antibacterial macrolones is reported, which features the use of a 4′-ester linked glycin for tethering the quinolone side chain to the macrolide scaffold. Among the analogs prepared, compounds 9e and 22f with a quinolon-6-yl moiety were found to have potent and well-balanced activity against clinically important respiratory tract pathogens, including erythromycin-susceptible and MLSB resistant strains of Streptococcus pneumoniae, Streptococcus pyogenes, and Haemophilus influenzae. In addition, potential lead compounds 9e and 22f demonstrated outstanding levels of activity against Moraxella catarrhalis and inducibly MLSB resistant Staphylococcus aureus. The best member of this series 22f rivals or exceeds, in potency, some of the most active ketolide antibacterial agents known today, such as telithromycin and cethromycin.
- Pavlovi?, Dra?en,Mutak, Stjepan
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p. 1255 - 1267
(2016/03/01)
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- COMPOUNDS
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The present invention relates to compounds of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical microbial infections in a human or animal body.
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- NOVEL 14 AND 15 MEMBERED-RING COMPOUNDS
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The present invention relates to 14- or 15-membered macrolides substituted at the 4" position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical microbial infections in a human or animal body.
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- MACROLIDES SUBSTITUTED AT THE 3-POSITION HAVING ANTIMICROBIAL ACTIVITY
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The present invention relates to 14- or 15-membered macrolides substituted at the 3-position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topi
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