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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
4
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pubmed:dateCreated |
2010-2-15
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pubmed:abstractText |
Efforts to refine the SAR of the piperazinyl-glutamate-pyridines for more potent analogs with improved pharmacokinetic profiles are described. Exploring substituted piperidines and other ring systems at the 4-pyridyl position led to compounds with improved potency and pharmacokinetic properties over candidate I. In particular, compounds 4t and 5t were discovered with a 10-fold improvement over potency and improved pharmacokinetic profiles in both the rat and dog.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Fibrinolytic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Glutamic Acid,
http://linkedlifedata.com/resource/pubmed/chemical/P2RY12 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/P2ry12 protein, rat,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Purinergic P2 Receptor Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Purinergic P2Y12
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BurneyMary WMW,
pubmed-author:CaseBrenda LBL,
pubmed-author:EnnisMichael DMD,
pubmed-author:GirardThomas JTJ,
pubmed-author:HallKerri AKA,
pubmed-author:HarrisPeter KPK,
pubmed-author:HiebschRonald RRR,
pubmed-author:HuffRita MRM,
pubmed-author:LachanceRhonda MRM,
pubmed-author:MischkeDeborah ADA,
pubmed-author:ParlowJohn JJJ,
pubmed-author:RappStephen RSR,
pubmed-author:WoerndleRhonda SRS
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pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1388-94
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:20097563-Administration, Oral,
pubmed-meshheading:20097563-Animals,
pubmed-meshheading:20097563-CHO Cells,
pubmed-meshheading:20097563-Cricetinae,
pubmed-meshheading:20097563-Cricetulus,
pubmed-meshheading:20097563-Dogs,
pubmed-meshheading:20097563-Fibrinolytic Agents,
pubmed-meshheading:20097563-Glutamic Acid,
pubmed-meshheading:20097563-Humans,
pubmed-meshheading:20097563-Inhibitory Concentration 50,
pubmed-meshheading:20097563-Molecular Structure,
pubmed-meshheading:20097563-Piperidines,
pubmed-meshheading:20097563-Platelet Aggregation,
pubmed-meshheading:20097563-Purinergic P2 Receptor Antagonists,
pubmed-meshheading:20097563-Pyridines,
pubmed-meshheading:20097563-Rats,
pubmed-meshheading:20097563-Receptors, Purinergic P2Y12,
pubmed-meshheading:20097563-Structure-Activity Relationship
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pubmed:year |
2010
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pubmed:articleTitle |
Part II: piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation.
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pubmed:affiliation |
Department of Medicinal Chemistry, Pfizer Global Research & Development, 700 Chesterfield Parkway West, Chesterfield, MO 63017, USA. john.j.parlow@pfizer.com
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pubmed:publicationType |
Journal Article
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