Title of article
p38 MAP kinase inhibitors. Part 5: Discovery of an orally bio-available and highly efficacious compound based on the 7-amino-naphthyridone scaffold
Author/Authors
Swaminathan R. Natarajan، نويسنده , , Luping Liu، نويسنده , , Mark Levorse، نويسنده , , James E. Thompson، نويسنده , , Edward A. O’Neill، نويسنده , , Stephen J. O’Keefe، نويسنده , , Kalpit A. Vora، نويسنده , , Raymond Cvetovich، نويسنده , , John Y. Chung، نويسنده , , Ester Carballo-Jane، نويسنده , , Denise M. Visco، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
4
From page
5468
To page
5471
Abstract
A new sub-class of p38 inhibitors represented by 7-amino-naphthyridone have been discovered. Benchmark compound 16 potently inhibited p38 in vitro, was functionally active, and displayed excellent pharmacokinetic profiles in two animal species. Compound 16 reduced inflammation in animal disease models at EC50 doses as low as 0.2 mpk.
Keywords
7-Amino-naphthyridones , p38 MAP kinase inhibitors , Peptide flip , Rat LPS challenge
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797409
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