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1. p38alpha mitogen-activated protein kinase inhibitors: optimization of a series of biphenylamides to give a molecule suitable for clinical progression.

Author

Aston NM, Bamborough P, Buckton JB, Edwards CD, Holmes DS, Jones KL, Patel VK, Smee PA, Somers DO, Vitulli G, and Walker AL

Subjects
Administration, Oral, Amides administration & dosage, Amides therapeutic use, Animals, Arthritis, Experimental drug therapy, Humans, Mice, Mitogen-Activated Protein Kinase 14 chemistry, Models, Molecular, Molecular Conformation, Protein Kinase Inhibitors administration & dosage, Protein Kinase Inhibitors therapeutic use, Rats, Amides chemistry, Amides pharmacology, Biphenyl Compounds chemistry, Drug Discovery, Mitogen-Activated Protein Kinase 14 antagonists & inhibitors, Protein Kinase Inhibitors chemistry, Protein Kinase Inhibitors pharmacology
Abstract

p38alpha MAP kinase is a key anti-inflammatory target for rheumatoid arthritis, influencing biosynthesis of pro-inflammatory cytokines TNFalpha and IL-1beta at a translational and transcriptional level. In this paper, we describe how we have optimized a series of novel p38alpha/beta inhibitors using crystal structures of our inhibitors bound to p38alpha, classical medicinal chemistry, and modeling of virtual libraries to derive a molecule suitable for progression into clinical development.

Published
2009
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