ArticleACS medicinal chemistry letters2011
Discovery of 4''-ether linked azithromycin-quinolone hybrid series: influence of the central linker on the antibacterial activity.
Article in ACS medicinal chemistry letters, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed.
- Benzoxaborole-modified azithromycins inhibit translation without inducingAntimicrobial agents and chemotherapy · 2026Article
- Hybrids/Conjugates/Chimera Drugs-Antimicrobial Hybrids: Antibiotics, Antifungals, Antituberculars, Antimalarials.Current medicinal chemistry · 2026Review
- Macrolones target bacterial ribosomes and DNA gyrase and can evade resistance mechanisms.Nature chemical biology · 2024Article
- Synthetic macrolides overcoming MLSCell discovery · 2024Article
- Hybrid Molecules of Azithromycin with Chloramphenicol and Metronidazole: Synthesis and Study of Antibacterial Properties.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Design, Synthesis and Biological Evaluation of Conjugates of 3-Molecules (Basel, Switzerland) · 2023Article
- Fluoroquinolones Hybrid Molecules as Promising Antibacterial Agents in the Fight against Antibacterial Resistance.Pharmaceutics · 2022Review
- Modifications of quinolones and fluoroquinolones: hybrid compounds and dual-action molecules.Monatshefte fur chemie · 2018Review
- Synthesis and Antibacterial Evaluation of a Series of 11,12-Cyclic Carbonate Azithromycin-3-O-descladinosyl-3-O-carbamoyl Glycosyl Derivatives.Molecules (Basel, Switzerland) · 2017Article
- Synthesis and Structure-Activity Relationships of α-Amino-γ-lactone Ketolides: A Novel Class of Macrolide Antibiotics.ACS medicinal chemistry letters · 2014Article
Corrections and comments
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Authors and funding
2 authors.
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Abstract
A series of novel C-4''-substituted azithromycins was synthesized and evaluated for in vitro antibacterial activity against a panel of representative erythromycin-susceptible and macrolide-lincosamide-streptogramin (MLS) resistant pathogens. In summary, azithromycin and quinolone substructures merged in a mutually SAR-compatible design gave rise to a new class of antimicrobials with an improved spectrum and potency over azithromycin. Prototypical analogues 7f and 8f display an improved potency versus azithromycin against Gram-positive and fastidious Gram-negative pathogens. In particular, these new leads maintain activity against MLS-resistant strains of Streptococcus pneumoniae and Streptococcus pyogenes. In addition, they represent an improvement over telithromycin (1) and cethromycin (2) against the fastidious Gram-negative pathogen Haemophilus influenzae.
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Registered trials
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