N-Terminal guanidine derivatives of teicoplanin antibiotics strongly active against glycopeptide resistant Enterococcus faecium
| Autor: | Pál Herczegh, Zsuzsanna Dombrádi, Zsolt Szűcs, Gyula Batta, Ilona Bereczki, Erzsébet Rőth, Márton Milánkovits, Eszter Ostorházi, Lajos Nagy, Anikó Borbás |
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| Rok vydání: | 2020 |
| Předmět: |
0301 basic medicine
medicine.drug_class 030106 microbiology Antibiotics Enterococcus faecium Microbial Sensitivity Tests Glycopeptide antibiotic Gram-Positive Bacteria 01 natural sciences Guanidines Microbiology 03 medical and health sciences chemistry.chemical_compound Antibiotic resistance Drug Discovery medicine Humans Guanidine Gram-Positive Bacterial Infections Pharmacology biology 010405 organic chemistry Teicoplanin Glycopeptides Drug Resistance Microbial biochemical phenomena metabolism and nutrition biology.organism_classification 0104 chemical sciences Anti-Bacterial Agents chemistry bacteria Antibacterial activity Bacteria medicine.drug |
| Zdroj: | The Journal of antibiotics. 73(9) |
| ISSN: | 1881-1469 |
| Popis: | Antibiotic resistance is one of the major challenges in healthcare of our time. To meet this challenge, we designed and prepared guanidine and lipophilic guanidine derivatives of the glycopeptide antibiotic teicoplanin to armed them with activity against the most threatening nosocomial bacteria, multiresistant enterococci. From teicoplanin and its pseudoaglycone, a series of N-terminal guanidine derivatives have been prepared with free and amide C-terminal parts. Six aliphatic and aromatic lipophilic carbodiimides were prepared and used for the synthesis of lipophilic guanidine teicoplanin conjugates. All new N-terminal guanidine antibiotics showed high activity against a standard panel of Gram-positive bacteria. Four selected derivatives displayed excellent antibacterial activity against a series of nosocomial VanA Enterococcus faecium strains. |
| Databáze: | OpenAIRE |
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