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Pubmed ID :12482439
Publication Date : //

Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.


The development of potent, orally bioavailable (in rat) and selective dihydroquinazolinone inhibitors of p38alpha MAP kinase is described. These analogues are hybrids of a pyridinylimidazole p38alpha inhibitor reported by Merck Research Laboratories and VX-745. Optimization of the C-5 phenyl and the C-7 piperidinyl substituents led to the identification of 15i which gave excellent suppression of TNF-alpha production in LPS-stimulated whole blood (IC(50)=10nM) and good oral exposure in rats (F=68%, AUCn PO=0.58 microM h).

Authors : Stelmach John E , Liu Luping , Patel Sangita B , Pivnichny James V , Scapin Giovanna , Singh Suresh , Hop Cornelis E C A , Wang Zhen , Strauss John R , Cameron Patricia M , Nichols Elizabeth A , O'Keefe Stephen J , O'Neill Edward A , Schmatz Dennis M , Schwartz Cheryl D , Thompson Chris M , Zaller Dennis M , Doherty James B ,

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