Novel antibiotics for the treatment of gram-positive bacterial infections
| Autor: | Siegfried Raddatz, Armin de Meijere, Viktor V. Sokolov, Gahlmann Reinhold, Jochen Krüger, Vladimir N. Belov, Rainer Endermann, Shamil Nizamov, Michael Brands, Jürgen Stoltefuss |
|---|---|
| Rok vydání: | 2002 |
| Předmět: |
Micrococcaceae
medicine.drug_class Staphylococcus Antibiotics Microbial Sensitivity Tests Pyrimidinones 010402 general chemistry medicine.disease_cause Arginine Gram-Positive Bacteria 01 natural sciences Guanidines Enterococcus faecalis Mice Structure-Activity Relationship Sepsis Drug Discovery medicine Animals Antibacterial agent biology 010405 organic chemistry Chemistry Dipeptides biology.organism_classification Methicillin-resistant Staphylococcus aureus 3. Good health 0104 chemical sciences Anti-Bacterial Agents Streptococcus pneumoniae Biochemistry Staphylococcus aureus Molecular Medicine Female Antibacterial activity Bacteria |
| Zdroj: | Journal of medicinal chemistry. 45(19) |
| ISSN: | 0022-2623 |
| Popis: | The natural dipeptide antibiotic TAN 1057 A,B displays excellent antibacterial activity against staphylococci including methicillin resistant Staphylococcus aureus. However, the in vitro activity against additional Gram-positive strains, in particular pneumococci and Enterococcus faecalis, proved to be considerably lower. We report the synthesis and pharmacological evaluation of new derivatives of this natural product that displayed increased antibacterial potency against staphylococci and were also active against pneumococci. In particular, the analogues bearing modified beta-homoarginine side chains with methylated guanidine moieties were shown to be significantly more potent than the natural product TAN 1057 A,B. |
| Databáze: | OpenAIRE |
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