title: The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.
abstract: A series of pyrazolo[1,5-a]pyridine derivatives was designed and synthesized as novel potent p38 kinase inhibitors. Our approaches towards improving in vitro metabolism and in vivo pharmacokinetic properties of the series are described.
authors.affiliation: GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA. mui.h.cheung@gsk.com
authors.forename: Mui
authors.initials: M
authors.lastname: Cheung
authors.forename: Philip A
authors.initials: PA
authors.lastname: Harris
authors.forename: Jennifer G
authors.initials: JG
authors.lastname: Badiang
authors.forename: Gregory E
authors.initials: GE
authors.lastname: Peckham
authors.forename: Stanley D
authors.initials: SD
authors.lastname: Chamberlain
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Alberti
authors.forename: David K
authors.initials: DK
authors.lastname: Jung
authors.forename: Stephanie S
authors.initials: SS
authors.lastname: Harris
authors.forename: Neal H
authors.initials: NH
authors.lastname: Bramson
authors.forename: Andrea H
authors.initials: AH
authors.lastname: Epperly
authors.forename: Stephen A
authors.initials: SA
authors.lastname: Stimpson
authors.forename: Michael R
authors.initials: MR
authors.lastname: Peel
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000494:pharmacology; D019540:Area Under Curve; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004285:Dogs; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D006801:Humans; D020128:Inhibitory Concentration 50; D007963:Leukocytes, Mononuclear / Q000187:drug effects; D020935:MAP Kinase Signaling System; D011725:Pyridines / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D051381:Rats; D013329:Structure-Activity Relationship; D048051:p38 Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000893:Anti-Inflammatory Agents; D004791:Enzyme Inhibitors; D011725:Pyridines; D048051:p38 Mitogen-Activated Protein Kinases