Publication Abstract from PubMed
p38 inhibitors based on 3,4-dihydropyrido[4,3-d]pyrimidazin-2-one template were synthesized and their SAR explored. Benchmark compounds 30, 35, and 36 were found to be potent against the enzyme. Crystal structure of p38 in complex with 30 indicated a key pi-stacking interaction with the pendant tyrosine residue-35 in the glycine-rich loop.
p38 MAP kinase inhibitors. Part 6: 2-arylpyridazin-3-ones as templates for inhibitor design.,Natarajan SR, Heller ST, Nam K, Singh SB, Scapin G, Patel S, Thompson JE, Fitzgerald CE, O'Keefe SJ Bioorg Med Chem Lett. 2006 Nov 15;16(22):5809-13. Epub 2006 Aug 30. PMID:16945533[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
