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Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors

Authors :
Dyckman, Alaric J.
Li, Tianle
Pitt, Sidney
Zhang, Rosemary
Shen, Ding Ren
McIntyre, Kim W.
Gillooly, Kathleen M.
Shuster, David J.
Doweyko, Arthur M.
Sack, John S.
Kish, Kevin
Kiefer, Susan E.
Newitt, John A.
Zhang, Hongjian
Marathe, Punit H.
McKinnon, Murray
Barrish, Joel C.
Dodd, John H.
Schieven, Gary L.
Leftheris, Katerina
Source :
Bioorganic & Medicinal Chemistry Letters. Aug2011, Vol. 21 Issue 15, p4633-4637. 5p.
Publication Year :
2011

Abstract

Abstract: Pyrrolo[2,1-f][1,2,4]triazine based inhibitors of p38α have been prepared exploring functional group modifications at the C6 position. Incorporation of aryl and heteroaryl ketones at this position led to potent inhibitors with efficacy in in vivo models of acute and chronic inflammation. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
21
Issue :
15
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
62843700
Full Text :
https://doi.org/10.1016/j.bmcl.2011.05.091