Bioorganic & Medicinal Chemistry Letters 2003-11-17

SAR of 3,4-dihydropyrido[3,2-d]pyrimidone p38 inhibitors.

Luping Liu, John E Stelmach, Swaminathan R Natarajan, Meng-Hsin Chen, Suresh B Singh, Cheryl D Schwartz, Catherine E Fitzgerald, Stephen J O'Keefe, Dennis M Zaller, Dennis M Schmatz, James B Doherty

Index: Bioorg. Med. Chem. Lett. 13(22) , 3979-82, (2003)

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Abstract

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.