Novel Antibacterial Class: A Series of Tetracyclic Derivatives
| Autor: | Niru B. Soni, Rolf Wagner, Steve D. Pratt, Teresa A. Rosenberg, Linda E. Chovan, Darlene J. Balli, Candace Black-Schaefer, Angela M. Nilius, Philip J. Merta, Moshe Weitzberg, Mira M. Hinman, Bruce A. Beutel, Frank L. Wagenaar, Douglas Kalvin |
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| Rok vydání: | 2006 |
| Předmět: |
Stereochemistry
Microbial Sensitivity Tests Heterocyclic Compounds 4 or More Rings Chemical synthesis Structure-Activity Relationship Drug Resistance Bacterial Drug Discovery Prokaryotic translation Humans Naphthyridines Cytotoxicity Antibacterial agent B-Lymphocytes biology Chemistry Stereoisomerism Translation (biology) biology.organism_classification In vitro Anti-Bacterial Agents Streptococcus pneumoniae Biochemistry Protein Biosynthesis Molecular Medicine Antibacterial activity Bacteria |
| Zdroj: | Journal of Medicinal Chemistry. 49:4842-4856 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm060010w |
| Popis: | We describe the synthesis and antibacterial activity of a series of tetracyclic naphthyridones. The members of this series act primarily via inhibition of bacterial translation and belong to the class of novel ribosome inhibitors (NRIs). In this paper we explore the structure-activity relationships (SAR) of these compounds to measure their ability both to inhibit bacterial translation and also to inhibit the growth of bacterial cells in culture. The most active of these compounds inhibit Streptococcus pneumoniae translation at concentrations of5 microM and have minimum inhibitory concentrations (MICs) of8 microg/mL against clinically relevant strains of bacteria. |
| Databáze: | OpenAIRE |
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