|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
3
|
|
pubmed:dateCreated |
2011-2-1
|
|
pubmed:abstractText |
Installation of sites for metabolism in the lead compound PHA-767408 was the key focus of the IKK-2 inhaled program. This paper reports our efforts to identify a novel series of aminopyridinecarboxamide-based IKK-2 inhibitors, which display low nanomolar potency against IKK-2 with long duration of action (DOA), and metabolically labile to phase I and/or phase II metabolizing enzymes with potential capability for multiple routes of clearance. Several compounds have demonstrated their potential usefulness in the treatment of asthma and chronic obstructive pulmonary disease (COPD).
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Aminopyridines,
http://linkedlifedata.com/resource/pubmed/chemical/I-kappa B Kinase,
http://linkedlifedata.com/resource/pubmed/chemical/Indazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Isonicotinic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Niacinamide,
http://linkedlifedata.com/resource/pubmed/chemical/PHA 408,
http://linkedlifedata.com/resource/pubmed/chemical/Phenethylamines,
http://linkedlifedata.com/resource/pubmed/chemical/Potassium Channel Blockers,
http://linkedlifedata.com/resource/pubmed/chemical/Protein Kinase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Sulfonamides,
http://linkedlifedata.com/resource/pubmed/chemical/dofetilide
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Feb
|
|
pubmed:issn |
1464-3391
|
|
pubmed:author |
pubmed-author:BonarSheri LSL,
pubmed-author:BrustkernSarah JSJ,
pubmed-author:ChenNatalie XNX,
pubmed-author:ChristineLoriL,
pubmed-author:HeierRichard FRF,
pubmed-author:HuYidingY,
pubmed-author:HuangHorng-ChihHC,
pubmed-author:KishoreNandini NNN,
pubmed-author:KurumbailRavi GRG,
pubmed-author:LennonPatrick JPJ,
pubmed-author:MathialaganSumathyS,
pubmed-author:PodaGennadiy IGI,
pubmed-author:RedingMatthew TMT,
pubmed-author:SelnessShaun RSR,
pubmed-author:SommersCynthia DCD,
pubmed-author:TUIP CPC,
pubmed-author:VenkatramanNeetuN,
pubmed-author:WolfsonSerge GSG,
pubmed-author:XiongLiL
|
|
pubmed:copyrightInfo |
Copyright © 2010 Elsevier Ltd. All rights reserved.
|
|
pubmed:issnType |
Electronic
|
|
pubmed:day |
1
|
|
pubmed:volume |
19
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
1242-55
|
|
pubmed:meshHeading |
pubmed-meshheading:21236687-Administration, Inhalation,
pubmed-meshheading:21236687-Aminopyridines,
pubmed-meshheading:21236687-Asthma,
pubmed-meshheading:21236687-Binding, Competitive,
pubmed-meshheading:21236687-Drug Design,
pubmed-meshheading:21236687-HEK293 Cells,
pubmed-meshheading:21236687-Humans,
pubmed-meshheading:21236687-I-kappa B Kinase,
pubmed-meshheading:21236687-Indazoles,
pubmed-meshheading:21236687-Isonicotinic Acids,
pubmed-meshheading:21236687-Microsomes, Liver,
pubmed-meshheading:21236687-Models, Molecular,
pubmed-meshheading:21236687-Molecular Structure,
pubmed-meshheading:21236687-Molecular Targeted Therapy,
pubmed-meshheading:21236687-Niacinamide,
pubmed-meshheading:21236687-Phenethylamines,
pubmed-meshheading:21236687-Potassium Channel Blockers,
pubmed-meshheading:21236687-Protein Kinase Inhibitors,
pubmed-meshheading:21236687-Pulmonary Disease, Chronic Obstructive,
pubmed-meshheading:21236687-Pyrazoles,
pubmed-meshheading:21236687-Structure-Activity Relationship,
pubmed-meshheading:21236687-Sulfonamides
|
|
pubmed:year |
2011
|
|
pubmed:articleTitle |
Aminopyridinecarboxamide-based inhaled IKK-2 inhibitors for asthma and COPD: Structure-activity relationship.
|
|
pubmed:affiliation |
Department of Medicinal Chemistry, Pfizer Inc., 700 Chesterfield Parkway West, St. Louis, MO 63017, USA. jin.xie@pfizer.com
|
|
pubmed:publicationType |
Journal Article
|
