Novel 3-deoxy-3-descladinosyl-6-O-methyl erythromycin a analogues. Synthesis and in vitro activity
| Autor: | Pauline M. Johnson, Angela M. Nilius, Daniel T. W. Chu, Daisy Pireh, Yat Sun Or, Robert K. Flamm, Richard L. Elliott, Jacob J. Plattner |
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| Rok vydání: | 1997 |
| Předmět: |
Carbamate
biology Stereochemistry Gram-positive bacteria medicine.medical_treatment Organic Chemistry Clinical Biochemistry Pharmaceutical Science biology.organism_classification Oxime Biochemistry Chemical synthesis In vitro chemistry.chemical_compound chemistry Drug Discovery Tributyltin medicine Molecular Medicine Antibacterial activity Molecular Biology Antibacterial agent |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 7:641-646 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(97)00078-4 |
| Popis: | A series of novel 3-deoxy-3-des-cladinosyl-6- O -methyl erythromycin A analogues has been synthesized and evaluated in vitro for antibacterial activity. These analogues were readily synthesized by tributyltin hydride-mediated radical reduction of a 3- O -xanthyl intermediate to afford the 3-deoxy macrolide. A number of oxime, carbonate, and carbamate derivatives were synthesized and evaluated for antibacterial activity. Overall, these analogues had fairly good antibacterial activity against gram-positive bacteria, although they were generally less potent than the corresponding 3- O -cladinosyl or 3-keto analogues. A series of novel 3-deoxy-3-des-cladinosyl-6- O -methyl erythromycin A analogues has been synthesized and evaluated in vitro for antibacterial activity. These analogues were readily synthesized by tributyltin hydride-mediated radical reduction of the 3- O -xanthyl intermediate to afford the 3-deoxy macrolide. A number of oxime, carbonate, and carbamate derivatives were synthesized and evaluated for antibacterial activity. Overall, these analogues had fairly good antibacterial activity against gram-positive bacteria, although they were generally less potent than the corresponding 3- O -cladinosyl or 3-keto analogues. |
| Databáze: | OpenAIRE |
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