Abstract
In this paper, we present the synthesis and SAR as well as selectivity, pharmacokinetic, and infection model data for representative analogues of a novel series of potent antibacterial LpxC inhibitors represented by hydroxamic acid.
MeSH terms
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Amidohydrolases / antagonists & inhibitors*
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Animals
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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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Biphenyl Compounds / chemical synthesis*
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Biphenyl Compounds / chemistry
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Biphenyl Compounds / pharmacology
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Catalytic Domain
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Crystallography, X-Ray
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Drug Resistance, Bacterial
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Hydrogen Bonding
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Hydroxamic Acids / chemical synthesis*
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Hydroxamic Acids / chemistry
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Hydroxamic Acids / pharmacology
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Mice
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Models, Molecular
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Molecular Conformation
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Phenyl Ethers / chemical synthesis*
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Phenyl Ethers / chemistry
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Phenyl Ethers / pharmacology
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Pseudomonas Infections / drug therapy*
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Pseudomonas aeruginosa
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Rats
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Stereoisomerism
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Structure-Activity Relationship
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Sulfides / chemical synthesis*
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Sulfides / chemistry
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Sulfides / pharmacology
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Sulfones / chemical synthesis*
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Sulfones / chemistry
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Sulfones / pharmacology
Substances
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Anti-Bacterial Agents
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Biphenyl Compounds
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Hydroxamic Acids
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Phenyl Ethers
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Sulfides
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Sulfones
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Amidohydrolases
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LpxC deacetylase, Pseudomonas
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UDP-3-O-acyl-N-acetylglucosamine deacetylase