Synthesis and Structural Characterisation of Selective Non-Carbohydrate-Based Inhibitors of Bacterial Sialidases
| Autor: | Garry L. Taylor, Paul Brear, Nicholas J. Westwood, Judith C. Telford |
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| Rok vydání: | 2012 |
| Předmět: |
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Molecular Drug media_common.quotation_subject Neuraminidase Human pathogen Biology Crystallography X-Ray Sialidase medicine.disease_cause Biochemistry Microbiology Structure-Activity Relationship chemistry.chemical_compound Streptococcus pneumoniae medicine Enzyme Inhibitors Molecular Biology Pathogen media_common chemistry.chemical_classification Molecular Structure Organic Chemistry medicine.disease Sialic acid Enzyme chemistry Molecular Medicine Sulfonic Acids Pneumonia (non-human) Hymecromone |
| Zdroj: | ChemBioChem. 13:2374-2383 |
| ISSN: | 1439-4227 |
| Popis: | The major human pathogen Streptococcus pneumoniae plays a key role in several disease states including septicaemia, meningitis and community-acquired pneumonia. Although vaccines against S. pneumoniae are available as prophylactics, there remains a need to identify and characterise novel chemical entities that can treat the diseases caused by this pathogen. S. pneumoniae expresses three sialidases, enzymes that cleave sialic acid from carbohydrate-based surface molecules. Two of these enzymes, NanA and NanB, have been implicated in the pathogenesis of S. pneumoniae and are considered to be validated drug targets. Here we report our studies on the synthesis and structural characterisation of novel NanB-selective inhibitors that are inspired by the β-amino-sulfonic acid family of buffers. |
| Databáze: | OpenAIRE |
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