Small Molecule p38 Inhibitors: Novel Structural Features and Advances from 2002-2005

Author(s): John Hynes, Jr., Katerina Leftheris.

Journal Name: Current Topics in Medicinal Chemistry

Volume 5 , Issue 10 , 2005

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The discovery and development of selective, efficacious, and safe small molecule p38 mitogen-activated protein kinase inhibitors for the treatment of inflammatory diseases remains the focus of many pharmaceutical research programs. Advances in small molecule p38 inhibitor design in potency and oral efficacy have been accelerated with the large number of available inhibitor-enzyme x-ray structures. These advances have allowed for the discovery of diverse sets of inhibitors with the opportunity to map inhibitor interactions and design selective inhibitors. This review covers recent compound disclosures in the patent and published literature over the last three years. Many disclosures represent new chemotypes as well as creative modifications of known structures.

Keywords: mitogen activated protein (map), rheumatoid arthritis, aniline hydroxamates, x-ray crystallography, cyanopyrimidine, indole-amides

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Article Details

Year: 2005
Page: [967 - 985]
Pages: 19
DOI: 10.2174/1568026054985920
Price: $58

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