'Reverse' alpha-ketoamide-based p38 MAP kinase inhibitors.
We have identified a second series of potent p38 inhibitors. As with our first generation series, these compounds are based on an alpha-ketoamide scaffold. The reversal of the ketoamide order, however, introduces more chemical flexibility and in addition results in improve potencies against p38.
Drug Discovery, Kemia, Inc., 5871 Oberlin Drive, Suite 100, San Diego, CA 92121, USA. catalaba@hotmail.com
Antonio Garrido
AG
Montalban
Erik
E
Boman
Chau-Dung
CD
Chang
Susana Conde
SC
Ceide
Russell
R
Dahl
David
D
Dalesandro
Nancy G J
NG
Delaet
Eric
E
Erb
Andrew
A
Gibbs
Jeff
J
Kahl
Linda
L
Kessler
Jan
J
Lundström
Stephen
S
Miller
Hiroshi
H
Nakanishi
Ed
E
Roberts
Eddine
E
Saiah
Robert
R
Sullivan
Zhijun
Z
Wang
Christopher J
CJ
Larson
D000495:Allosteric Site; D000577:Amides / Q000737:chemistry*; D000893:Anti-Inflammatory Agents / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods; D016207:Cytokines / Q000378:metabolism; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D007249:Inflammation / Q000188:drug therapy; D020128:Inhibitory Concentration 50; D007659:Ketones / Q000737:chemistry*; D008956:Models, Chemical; D008958:Models, Molecular; D013329:Structure-Activity Relationship; D048051:p38 Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors*
D000577:Amides; D000893:Anti-Inflammatory Agents; D016207:Cytokines; D004791:Enzyme Inhibitors; D007659:Ketones; D048051:p38 Mitogen-Activated Protein Kinases