Abstract
Our research on hydantoin based TNF-α converting enzyme (TACE) inhibitors has led to an acetylene containing series that demonstrates sub-nanomolar potency (K(i)) as well as excellent activity in human whole blood. These studies led to the discovery of highly potent TACE inhibitors with good DMPK profiles.
Published by Elsevier Ltd.
MeSH terms
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ADAM Proteins / antagonists & inhibitors*
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ADAM Proteins / metabolism
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ADAM17 Protein
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Acetylene / analogs & derivatives
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Acetylene / pharmacokinetics
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Acetylene / therapeutic use
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Animals
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Anti-Inflammatory Agents / chemistry*
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Anti-Inflammatory Agents / pharmacokinetics
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Anti-Inflammatory Agents / therapeutic use
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Arthritis, Rheumatoid / drug therapy*
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Dogs
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Haplorhini
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Humans
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Protease Inhibitors / chemistry*
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Protease Inhibitors / pharmacokinetics
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Protease Inhibitors / therapeutic use
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Rats
Substances
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Anti-Inflammatory Agents
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Protease Inhibitors
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ADAM Proteins
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ADAM17 Protein
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ADAM17 protein, human
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Adam17 protein, rat
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Acetylene