Abstract
A series of borinic acid picolinate esters were synthesized and screened for their minimum inhibitory concentration (MIC) against Gram-positive and -negative bacteria. Our lead compounds were then screened for anti-inflammatory activity. From these studies, we identified 3-hydroxypyridine-2-carbonyloxy-bis(3-chloro-4-methylphenyl)borane (2g, AN0128) as having the best combination of anti-bacterial and anti-inflammatory activities. This compound is now in clinical development for dermatological conditions.
MeSH terms
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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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Anti-Inflammatory Agents / chemical synthesis*
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Anti-Inflammatory Agents / chemistry
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Anti-Inflammatory Agents / pharmacology*
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Boranes / chemical synthesis*
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Boranes / chemistry
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Boranes / pharmacology*
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Boron / chemistry*
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Boron Compounds / chemistry
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Cytokines / metabolism
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Esters / chemistry
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Humans
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Leukocytes / drug effects
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Leukocytes / metabolism
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Molecular Structure
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Pyridines / chemical synthesis*
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Pyridines / chemistry
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Pyridines / pharmacology*
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Skin Diseases / drug therapy
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Structure-Activity Relationship
Substances
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3-hydroxypyridine-2-carbonyloxy-bis(3-chloro-4-methylphenyl)borane
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Anti-Bacterial Agents
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Anti-Inflammatory Agents
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Boranes
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Boron Compounds
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Cytokines
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Esters
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Pyridines
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diphenylborate
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Boron