Title of article :
p38 MAP 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
Author/Authors :
Swaminathan R. Natarajan، نويسنده , , David D. Wisnoski، نويسنده , , Suresh B. Singh، نويسنده , , John E. Stelmach، نويسنده , , Edward A. OʹNeill، نويسنده , , Cheryl D. Schwartz، نويسنده , , Chris M. Thompson، نويسنده , , Catherine E. Fitzgerald، نويسنده , , Stephen J. OʹKeefe، نويسنده , , Sanjeev Kumar، نويسنده , , Cornelis E. C. A. Hop، نويسنده , , Dennis M. Zaller، نويسنده , , Dennis M. Schmatz، نويسنده , , James B. Doherty، نويسنده ,
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.
