Abstract
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
Current Topics in Medicinal Chemistry
Title: Small Molecule p38 Inhibitors: Novel Structural Features and Advances from 2002-2005
Volume: 5 Issue: 10
Author(s): John Hynes, Jr. and Katerina Leftheris
Affiliation:
Keywords: mitogen activated protein (map), rheumatoid arthritis, aniline hydroxamates, x-ray crystallography, cyanopyrimidine, indole-amides
Abstract: 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.
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Cite this article as:
Hynes, Jr. John and Leftheris Katerina, Small Molecule p38 Inhibitors: Novel Structural Features and Advances from 2002-2005, Current Topics in Medicinal Chemistry 2005; 5 (10) . https://dx.doi.org/10.2174/1568026054985920
DOI https://dx.doi.org/10.2174/1568026054985920 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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