Title of article
p38 MAP kinase inhibitors. Part 6: 2-Arylpyridazin-3-ones as templates for inhibitor design
Author/Authors
Swaminathan R. Natarajan، نويسنده , , Stephen T. Heller، نويسنده , , Kiyean Nam، نويسنده , , Suresh B. Singh، نويسنده , , Giovanna Scapin، نويسنده , , Sangita Patel، نويسنده , , James E. Thompson، نويسنده , , Catherine E. Fitzgerald، نويسنده , , Stephen J. O’Keefe، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
5809
To page
5813
Abstract
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 π-stacking interaction with the pendant tyrosine residue-35 in the glycine-rich loop.
Keywords
p38 Inhibitors , MAP kinase
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797479
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