Preparation of novel antibacterial agents. Replacement of the central aromatic ring with heterocycles
| Autor: | Douglas C. Rohrer, Cory M. Stiff, Jianke Li, Brian D. Wakefield, Keith R. Marotti, Michael T. Sweeney, Donna L. Romero, Gary E. Zurenko, J. Craig Ruble, Atli Thorarensen |
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| Rok vydání: | 2007 |
| Předmět: |
Clinical Biochemistry
Serum albumin Pharmaceutical Science Microbial Sensitivity Tests Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Heterocyclic Compounds Drug Discovery Anthranilic acid medicine Humans Potency Organic chemistry ortho-Aminobenzoates Molecular Biology Serum Albumin Antibacterial agent Bacteria biology Organic Chemistry Biological activity Human serum albumin Anti-Bacterial Agents body regions chemistry embryonic structures biology.protein Molecular Medicine Antibacterial activity Protein Binding medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 17:2347-2350 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2006.12.055 |
| Popis: | Discovery of novel antibacterial agents is a significant challenge. We have recently reported on our discovery of novel antibacterial agents in which we have rapidly optimized potency utilizing a parallel chemistry approach. These advanced leads suffer from high affinity for human serum albumin (HSA). In an effort to decrease the affinity for HSA we have prepared a series of heterocyclic analogs, which retained antibacterial activity and demonstrated reduced affinity for HSA. |
| Databáze: | OpenAIRE |
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