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

Alaric J Dyckman Tianle Li Sidney Pitt Rosemary Zhang Ding Ren Shen Kim W McIntyre Kathleen M Gillooly David J Shuster Arthur M Doweyko John S Sack Kevin Kish Susan E Kiefer John A Newitt Hongjian Zhang Punit H Marathe Murray McKinnon Joel C Barrish John H Dodd Gary L Schieven Katerina Leftheris

Bioorg Med Chem Lett

Bristol-Myers Squibb, Research and Development, Princeton, NJ 08543-4000, USA.

Published: August 2011

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.

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http://dx.doi.org/10.1016/j.bmcl.2011.05.091DOI Listing

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