The discovery and initial optimisation of pyrrole-2-carboxamides as inhibitors of p38alpha MAP kinase

A novel pyrrole-2-carboxamide series of p38alpha inhibitors, discovered through the application of virtual screening, is presented. Following evaluation of activity, selectivity and developability properties of commercially available analogues, a synthesis program enabled rapid assessment of the ser...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-07, Vol.20 (13), p.3936-3940
Main Authors: Down, Kenneth, Bamborough, Paul, Alder, Catherine, Campbell, Amanda, Christopher, John A, Gerelle, Maria, Ludbrook, Steve, Mallett, Dave, Mellor, Geoff, Miller, David D, Pearson, Rosannah, Ray, Keith, Solanke, Yemisi, Somers, Don
Format: Article
Language:English
Subjects:
Amides - chemical synthesis
Amides - chemistry
Amides - pharmacology
Dose-Response Relationship, Drug
Drug Discovery
High-Throughput Screening Assays
Molecular Structure
p38 Mitogen-Activated Protein Kinases - antagonists & inhibitors
Protein Kinase Inhibitors - chemical synthesis
Protein Kinase Inhibitors - chemistry
Protein Kinase Inhibitors - pharmacology
Pyrroles - chemistry
Stereoisomerism
Structure-Activity Relationship
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Summary:A novel pyrrole-2-carboxamide series of p38alpha inhibitors, discovered through the application of virtual screening, is presented. Following evaluation of activity, selectivity and developability properties of commercially available analogues, a synthesis program enabled rapid assessment of the series' suitability for further lead optimisation studies.
ISSN:1464-3405
DOI:10.1016/j.bmcl.2010.05.011