Synthesis and antibacterial activity of acylides (3-O-acyl-erythromycin derivatives): a novel class of macrolide antibiotics
| Autor: | Yoko Misawa, Tetsuya Tanikawa, Masakazu Sato, Toshifumi Asaka, Masato Kashimura, Shigeo Morimoto, Atsushi Nishida, Keiko Suzuki, Kazuya Kameo |
|---|---|
| Rok vydání: | 2001 |
| Předmět: |
Staphylococcus aureus
medicine.drug_class Stereochemistry Enterococcus faecium Erythromycin Microbial Sensitivity Tests medicine.disease_cause Enterococcus faecalis Microbiology Macrolide Antibiotics Mice Structure-Activity Relationship Drug Discovery Streptococcus pneumoniae medicine Animals Antibacterial agent biology Chemistry Staphylococcal Infections biology.organism_classification Streptococcaceae Anti-Bacterial Agents Molecular Medicine Antibacterial activity medicine.drug |
| Zdroj: | Journal of medicinal chemistry. 44(24) |
| ISSN: | 0022-2623 |
| Popis: | Introduction of an acyl group to the 3-O-position of erythromycin A derivatives instead of L-cladinose led to a novel class of macrolide antibiotics that we named "acylides". The 3-O-nitrophenylacetyl derivative TEA0777 showed significantly potent activity against not only erythromycin-susceptible Gram-positive pathogens but also inducibly macrolides-lincosamides-streptogramin B (MLS(B))-resistant Staphylococcus aureus and efflux-resistant Streptococcus pneumoniae. These results indicated that acylides have potential as next-generation macrolide antibiotics. |
| Databáze: | OpenAIRE |
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