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. Modif...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-11, Vol.13 (22), p.3979-3982
Hauptverfasser:	Liu, Luping, Stelmach, John E., Natarajan, Swaminathan R., Chen, Meng-Hsin, Singh, Suresh B., Schwartz, Cheryl D., Fitzgerald, Catherine E., O'Keefe, Stephen J., Zaller, Dennis M., Schmatz, Dennis M., Doherty, James B.
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Kinetics Medical sciences Mitogen-Activated Protein Kinases - antagonists & inhibitors Molecular Structure p38 Mitogen-Activated Protein Kinases Pharmacology. Drug treatments Pyrimidinones - chemical synthesis Pyrimidinones - pharmacology Structure-Activity Relationship
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Zusammenfassung:	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. 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 discussed.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2003.08.059