p38MAP kinase inhibitors. Part 1: design and development of a new class of potent and highly selective inhibitors based on 3, 4-dihydropyrido [3, 2-d] pyrimidone …

…, CM Thompson, CE Fitzgerald, SJ O'Keefe…

Index: Natarajan, Swaminathan R.; Wisnoski, David D.; Singh, Suresh B.; Stelmach, John E.; O'Neill, Edward A.; Schwartz, Cheryl D.; Thompson, Chris M.; Fitzgerald, Catherine E.; O'Keefe, Stephen J.; Kumar, Sanjeev; Hop, Cornelis E. C. A.; Zaller, Dennis M.; Schmatz, Dennis M.; Doherty, James B. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 2 p. 273 - 276

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Citation Number: 55

Abstract

A new class of p38 antagonists based on 3, 4-dihydropyrido [3, 2,-d] pyrimidine scaffold has been developed. These inhibitors exhibit unprecedented selectivity towards p38 over other very closely related kinases. Compounds 25, 33, and 34 were identified as benchmark analogues for follow-up studies. They show good potency for enzyme inhibition and excellent functional activity.