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.
Liu
Luping
L
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. luping_liu@merck.com
Stelmach
John E
JE
Natarajan
Swaminathan R
SR
Chen
Meng-Hsin
MH
Singh
Suresh B
SB
Schwartz
Cheryl D
CD
Fitzgerald
Catherine E
CE
O'Keefe
Stephen J
SJ
Zaller
Dennis M
DM
Schmatz
Dennis M
DM
Doherty
James B
JB
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