p38 Kinase inhibitors for the treatment of arthritis and osteoporosis: thienyl, furyl, and pyrrolyl ureas

Inhibitors of the MAP kinase p38 are potentially useful for the treatment for osteoporosis, arthritis, and other inflammatory diseases. A series of thienyl, furyl, and pyrrolyl ureas has been identified as potent p38 inhibitors, displaying in vitro activity in the nanomolar range.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2001-01, Vol.11 (1), p.9-12
Main Authors: Redman, Anikó M, Johnson, Jeffrey S, Dally, Robert, Swartz, Steve, Wild, Hanno, Paulsen, Holger, Caringal, Yolanda, Gunn, David, Renick, Joel, Osterhout, Martin, Kingery-Wood, Jill, Smith, Roger A, Lee, Wendy, Dumas, Jacques, Wilhelm, Scott M, Housley, Timothy J, Bhargava, Ajay, Ranges, Gerald E, Shrikhande, Alka, Young, Deborah, Bombara, Michael, Scott, William J
Format: Article
Language:English
Subjects:
Arthritis - drug therapy
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Enzyme Inhibitors - therapeutic use
Furans - chemical synthesis
Furans - chemistry
Furans - pharmacology
Furans - therapeutic use
Humans
Inhibitory Concentration 50
Interleukin-6 - antagonists & inhibitors
Interleukin-6 - metabolism
Medical sciences
Mitogen-Activated Protein Kinases - antagonists & inhibitors
Molecular Structure
Osteoporosis - drug therapy
p38 Mitogen-Activated Protein Kinases
Pharmacology. Drug treatments
Pyrroles - chemical synthesis
Pyrroles - chemistry
Pyrroles - pharmacology
Pyrroles - therapeutic use
Thiophenes - chemical synthesis
Thiophenes - chemistry
Thiophenes - pharmacology
Thiophenes - therapeutic use
Tumor Cells, Cultured
Urea - analogs & derivatives
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Description
Summary:Inhibitors of the MAP kinase p38 are potentially useful for the treatment for osteoporosis, arthritis, and other inflammatory diseases. A series of thienyl, furyl, and pyrrolyl ureas has been identified as potent p38 inhibitors, displaying in vitro activity in the nanomolar range.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00574-6