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2-Aminotetralones: novel inhibitors of MurA and MurZ
- Source :
- Bioorganic and Medicinal Chemistry Letters, Bioorganic and Medicinal Chemistry Letters, Elsevier, 2008, 18 (5), pp.1730-1734. ⟨10.1016/j.bmcl.2008.01.089⟩
- Publication Year :
- 2007
-
Abstract
- Several 2-aminotetralones were identified as novel inhibitors of the bacterial enzymes MurA and MurZ. A number of these inhibitors demonstrated antibacterial activity against Staphylococcus aureus and Escherichia coli with MICs in the range 8-128 microg/ml. Based on structure-activity relationships we propose that the alpha-aminoketone functionality is responsible for the inhibitory activity and evidence is provided to support a covalent mode of action involving the C115 thiol group of MurA/MurZ.
- Subjects :
- Models, Molecular
Staphylococcus aureus
[SDV]Life Sciences [q-bio]
Clinical Biochemistry
Pharmaceutical Science
Microbial Sensitivity Tests
medicine.disease_cause
Biochemistry
Microbiology
Structure-Activity Relationship
Mura
Bacterial Proteins
Drug Discovery
medicine
Escherichia coli
Structure–activity relationship
[CHIM]Chemical Sciences
[SDV.BBM]Life Sciences [q-bio]/Biochemistry, Molecular Biology
Mode of action
Molecular Biology
ComputingMilieux_MISCELLANEOUS
Antibacterial agent
Tetralones
chemistry.chemical_classification
Binding Sites
biology
Molecular Structure
[CHIM.ORGA]Chemical Sciences/Organic chemistry
Organic Chemistry
Anti-Bacterial Agents
Enzyme
chemistry
Enzyme inhibitor
biology.protein
Molecular Medicine
Antibacterial activity
[CHIM.RADIO]Chemical Sciences/Radiochemistry
Subjects
Details
- ISSN :
- 14643405 and 0960894X
- Volume :
- 18
- Issue :
- 5
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....d49ba11a238d8f507d44bd876fc535c8
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.01.089⟩