Synthesis and biological properties of a new series of anti-MRSA β-lactams; 2-(thiazol-2-ylthio)carbapenems
| Autor: | Hitoshi Houchigai, Hisatoshi Shinagawa, Yoshihiro Sumita, Makoto Sunagawa, Hiroshi Yamaga |
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| Rok vydání: | 1997 |
| Předmět: |
Models
Molecular Dipeptidases Staphylococcus aureus Carbapenem Magnetic Resonance Spectroscopy Stereochemistry Clinical Biochemistry Pharmaceutical Science Microbial Sensitivity Tests Anti mrsa Biochemistry Structure-Activity Relationship Biological property Drug Discovery β lactams Side chain medicine Humans Moiety Molecular Biology Serum Albumin Chemistry Organic Chemistry Cationic polymerization biochemical phenomena metabolism and nutrition Human serum albumin bacterial infections and mycoses In vitro Anti-Bacterial Agents Cephalosporins Carbapenems Models Chemical Molecular Medicine Methicillin Resistance Protein Binding medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry. 5:601-621 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/s0968-0896(96)00273-8 |
| Popis: | A series of 1β-methylcarbapenems containing variously C-2 substituted thiazol-2-ylthio groups were synthesized, and their in vitro anti-MRSA activity was examined. Among them, 1β-methyl-2-(4-arylthiazol-2-ylthio) carbapenems exhibited superior anti-MRSA activity. Introduction of a cationic moiety in the C-2 side chain not only reduced the binding to HSA but also increased the stability against DHP-I, without affecting the anti-MRSA activity. It was also found that the distance between the cationic moiety and the carbapenem skeleton was related to the strength of HSA binding and the stability against DHP-I. |
| Databáze: | OpenAIRE |
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