Abstract
Halopemide, which was identified by HTS to inhibit phospholipase D2 (PLD2), provided the basis for an exploratory effort to identify potent inhibitors of PLD2 for use as inflammatory mediators. Parallel synthesis and purification were utilized to rapidly identify orally available amide analogs derived from indole 2-carboxylic acids with superior potency versus PLD2.
MeSH terms
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Administration, Oral
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Amides
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Animals
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Anti-Inflammatory Agents
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Domperidone / analogs & derivatives*
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Domperidone / chemical synthesis
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Domperidone / pharmacokinetics
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacokinetics
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Inhibitory Concentration 50
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Pharmacokinetics
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Phospholipase D / antagonists & inhibitors*
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Rats
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Structure-Activity Relationship
Substances
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Amides
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Anti-Inflammatory Agents
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Enzyme Inhibitors
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Domperidone
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halopemide
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Phospholipase D