Abstract
A successful scaffold-hopping approach gave a novel series of inhibitors of bacterial glutamate racemase (MurI). Early SAR studies of the 8-benzyl pteridine-6,7-diones led to compounds with micromolar enzyme potency and antibacterial activity.
MeSH terms
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Amino Acid Isomerases / antagonists & inhibitors*
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Anti-Bacterial Agents / chemical synthesis*
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology*
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Combinatorial Chemistry Techniques
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Gram-Positive Bacteria / drug effects
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Gram-Positive Bacteria / enzymology*
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Microbial Sensitivity Tests
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Molecular Structure
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Pteridines / chemical synthesis*
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Pteridines / chemistry
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Pteridines / pharmacology*
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Structure-Activity Relationship
Substances
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8-benzyl pteridine-6,7-dione
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Anti-Bacterial Agents
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Pteridines
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Amino Acid Isomerases
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glutamate racemase