Abstract
3-Methoxybenzamide (1) is a weak inhibitor of the essential bacterial cell division protein FtsZ. Alkyl derivatives of 1 are potent antistaphylococcal compounds with suboptimal drug-like properties. Exploration of the structure-activity relationships of analogues of these inhibitors led to the identification of potent antistaphylococcal compounds with improved pharmaceutical properties.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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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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Bacterial Proteins / antagonists & inhibitors*
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Biological Availability
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Blood Proteins / metabolism
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Caco-2 Cells
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Cell Division / drug effects
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Cell Membrane Permeability
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Cytoskeletal Proteins / antagonists & inhibitors*
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Hepatocytes / metabolism
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Humans
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Mice
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Microbial Sensitivity Tests
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Models, Molecular
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Protein Binding
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Pyridines / chemical synthesis*
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Pyridines / chemistry
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Pyridines / pharmacology
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Staphylococcal Infections / drug therapy
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Staphylococcus aureus / cytology
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Staphylococcus aureus / drug effects*
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Structure-Activity Relationship
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Thiazoles / chemical synthesis*
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Thiazoles / chemistry
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Thiazoles / pharmacology
Substances
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Anti-Bacterial Agents
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Bacterial Proteins
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Blood Proteins
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Cytoskeletal Proteins
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FtsZ protein, Bacteria
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PC190723
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Pyridines
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Thiazoles