title: Synthesis and biological activity of pyridopyridazin-6-one p38 MAP kinase inhibitors. Part 1.
abstract: The development and synthesis of potent p38α MAP kinase inhibitors containing a pyridazinone platform is described. Evolution of the p38α selective pyridopyridazin-6-one series from the p38α/β dual inhibitor 2H-quinolizin-2-one series will be discussed in full detail.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. robert_tynebor@merck.com
authors.forename: Robert M
authors.initials: RM
authors.lastname: Tynebor
authors.forename: Meng-Hsin
authors.initials: MH
authors.lastname: Chen
authors.forename: Swaminathan R
authors.initials: SR
authors.lastname: Natarajan
authors.forename: Edward A
authors.initials: EA
authors.lastname: O'Neill
authors.forename: James E
authors.initials: JE
authors.lastname: Thompson
authors.forename: Catherine E
authors.initials: CE
authors.lastname: Fitzgerald
authors.forename: Stephen J
authors.initials: SJ
authors.lastname: O'Keefe
authors.forename: James B
authors.initials: JB
authors.lastname: Doherty
mesh_terms: D000818:Animals; D001665:Binding Sites; D020134:Catalytic Domain; D003198:Computer Simulation; D048308:Mitogen-Activated Protein Kinase 14 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D017434:Protein Structure, Tertiary; D011724:Pyridazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D047428:Protein Kinase Inhibitors; D011724:Pyridazines; D048308:Mitogen-Activated Protein Kinase 14