'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.
Montalban
Antonio Garrido
AG
Drug Discovery, Kemia, Inc., 5871 Oberlin Drive, Suite 100, San Diego, CA 92121, USA. catalaba@hotmail.com
Boman
Erik
E
Chang
Chau-Dung
CD
Ceide
Susana Conde
SC
Dahl
Russell
R
Dalesandro
David
D
Delaet
Nancy G J
NG
Erb
Eric
E
Gibbs
Andrew
A
Kahl
Jeff
J
Kessler
Linda
L
Lundström
Jan
J
Miller
Stephen
S
Nakanishi
Hiroshi
H
Roberts
Ed
E
Saiah
Eddine
E
Sullivan
Robert
R
Wang
Zhijun
Z
Larson
Christopher J
CJ
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