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The identification of pyrazolo[1,5- a]pyridines as potent p38 kinase inhibitors

A series of pyrazolo[1,5- a]pyridine derivatives was designed and synthesized as novel potent p38 kinase inhibitors. Our approaches towards improving in vitro metabolism and in vivo pharmacokinetic properties of the series are described. A series of pyrazolo[1,5- a]pyridine derivatives was designed...

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Published in:Bioorganic & medicinal chemistry 2008-10, Vol.18 (20), p.5428-5430
Main Authors: Cheung, Mui, Harris, Philip A., Badiang, Jennifer G., Peckham, Gregory E., Chamberlain, Stanley D., Alberti, Michael J., Jung, David K., Harris, Stephanie S., Bramson, Neal H., Epperly, Andrea H., Stimpson, Stephen A., Peel, Michael R.
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container_issue 20
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container_title Bioorganic & medicinal chemistry
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creator Cheung, Mui
Harris, Philip A.
Badiang, Jennifer G.
Peckham, Gregory E.
Chamberlain, Stanley D.
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Jung, David K.
Harris, Stephanie S.
Bramson, Neal H.
Epperly, Andrea H.
Stimpson, Stephen A.
Peel, Michael R.
description A series of pyrazolo[1,5- a]pyridine derivatives was designed and synthesized as novel potent p38 kinase inhibitors. Our approaches towards improving in vitro metabolism and in vivo pharmacokinetic properties of the series are described. A series of pyrazolo[1,5- a]pyridine derivatives was designed and synthesized as novel potent p38 kinase inhibitors. Our approaches towards improving in vitro metabolism and in vivo pharmacokinetic properties of the series are described.
doi_str_mv 10.1016/j.bmcl.2008.09.040
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identifier ISSN: 0960-894X
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source ScienceDirect Journals
subjects Animals
Anti-Inflammatory Agents - chemical synthesis
Anti-Inflammatory Agents - pharmacology
Area Under Curve
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Chemistry, Pharmaceutical - methods
Dogs
Drug Design
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - pharmacokinetics
Humans
Inhibitory Concentration 50
Leukocytes, Mononuclear - drug effects
MAP Kinase Signaling System
Medical sciences
p38 Inhibitor
p38 Mitogen-Activated Protein Kinases - antagonists & inhibitors
p38 Mitogen-Activated Protein Kinases - metabolism
Pharmacology. Drug treatments
Pyrazolopyridine
Pyridines - chemical synthesis
Pyridines - pharmacokinetics
Rats
Structure-Activity Relationship
title The identification of pyrazolo[1,5- a]pyridines as potent p38 kinase inhibitors
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