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 scaffold

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...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-01, Vol.13 (2), p.273-276
Hauptverfasser:	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
Format:	Artikel
Sprache:	eng
Schlagworte:	Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Indicators and Reagents Mitogen-Activated Protein Kinases - antagonists & inhibitors p38 Mitogen-Activated Protein Kinases Pyridines - chemical synthesis Pyridines - pharmacology Pyrimidinones - chemical synthesis Pyrimidinones - pharmacology Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0960-894X
DOI:	10.1016/S0960-894X(02)00876-4