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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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| Published in: | Bioorganic & medicinal chemistry letters 2010-07, Vol.20 (13), p.3936-3940 |
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| Main Authors: | , , , , , , , , , , , , , |
| Format: | Article |
| Language: | English |
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| container_end_page | 3940 |
| container_issue | 13 |
| container_start_page | 3936 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 20 |
| creator | 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 |
| description | 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. |
| doi_str_mv | 10.1016/j.bmcl.2010.05.011 |
| format | article |
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| fulltext | fulltext |
| identifier | EISSN: 1464-3405 |
| ispartof | Bioorganic & medicinal chemistry letters, 2010-07, Vol.20 (13), p.3936-3940 |
| issn | 1464-3405 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_748968384 |
| source | ScienceDirect Freedom Collection 2022-2024 |
| 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 |
| title | The discovery and initial optimisation of pyrrole-2-carboxamides as inhibitors of p38alpha MAP kinase |
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