Synthesis and biological properties of 4″-O-acyl derivatives of 8a-Aza-8a-homoerythromycin
| Autor: | Vlado, Stimac, Sulejman, Alihodzic, Gorjana, Lazarevski, Stjepan, Mutak, Zorica Marusic, Istuk, Andrea, Fajdetic, Ivana, Palej, Hana Cipcic, Paljetak, Natasa, Marsic, Jasna, Padovan, Branka, Tavcar, Vesna, Erakovic Haber |
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| Rok vydání: | 2009 |
| Předmět: |
Male
Magnetic Resonance Spectroscopy Gram-negative bacteria Stereochemistry Acylation azalide acylide antibacterial activity pharmacokinetics structure-activity relationship Stereoisomerism Azalide Gram-Positive Bacteria Catalysis Mass Spectrometry Structure-Activity Relationship In vivo Gram-Negative Bacteria Drug Discovery medicine Animals Structure–activity relationship Rats Wistar Pharmacology biology Chemistry biology.organism_classification Anti-Bacterial Agents Erythromycin Rats Bioavailability Indicators and Reagents Efflux medicine.drug |
| Zdroj: | The Journal of Antibiotics. 62:133-144 |
| ISSN: | 1881-1469 0021-8820 |
| DOI: | 10.1038/ja.2009.1 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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