SAR of 3,4-dihydropyrido[3,2-d]pyrimidone p38 inhibitors.
Development for a class of potent 3,4-dihydropyrido(3,2-d)pyrimidone inhibitors of p38a MAP kinase is described. Modification of N-1 aryl and C-6 arylsulfide in 3,4-dihydropyrido(3,2-d)pyrimidone analogues for the interaction with the hydrophobic pockets in p38 active site is also discussed.
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. luping_liu@merck.com
Luping
L
Liu
John E
JE
Stelmach
Swaminathan R
SR
Natarajan
Meng-Hsin
MH
Chen
Suresh B
SB
Singh
Cheryl D
CD
Schwartz
Catherine E
CE
Fitzgerald
Stephen J
SJ
O'Keefe
Dennis M
DM
Zaller
Dennis M
DM
Schmatz
James B
JB
Doherty
D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D007700:Kinetics; D020928:Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D048051:p38 Mitogen-Activated Protein Kinases
C487477:3,4-dihydropyrido(3,2-d)pyrimidone; D004791:Enzyme Inhibitors; D011744:Pyrimidinones; D020928:Mitogen-Activated Protein Kinases; D048051:p38 Mitogen-Activated Protein Kinases