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rdf:type |
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lifeskim:mentions |
umls-concept:C0205177,
umls-concept:C0205531,
umls-concept:C0226896,
umls-concept:C0302923,
umls-concept:C0442027,
umls-concept:C1328819,
umls-concept:C1335281,
umls-concept:C1527415,
umls-concept:C1611588,
umls-concept:C1709439,
umls-concept:C1880355,
umls-concept:C1999216
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pubmed:issue |
11
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pubmed:dateCreated |
2008-5-30
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|
pubmed:abstractText |
A series of quinoline/naphthalene-difluoromethylphosphonates were prepared and were found to be potent PTP1B inhibitors. Most of these compounds bearing polar functionalities or large lipophilic residues did not show appreciable oral bioavailability in rodents while small and less polar analogs displayed moderate to good oral bioavailability. The title compound was found to have the best overall potency and pharmacokinetic profile and was found to be efficacious in animal models of diabetes and cancer.
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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 |
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pubmed:status |
MEDLINE
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|
pubmed:month |
Jun
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BaylyChristopher ICI,
pubmed-author:BelleyMichelM,
pubmed-author:ChanChi-ChungCC,
pubmed-author:ColucciJohnJ,
pubmed-author:DufresneClaudeC,
pubmed-author:GirouxAndreA,
pubmed-author:HanYongxinY,
pubmed-author:KennedyBrian PBP,
pubmed-author:LauCheuk KCK,
pubmed-author:LeblancYvesY,
pubmed-author:McKayDanielD,
pubmed-author:ScapinGiovanaG,
pubmed-author:SkoreyKathrynK,
pubmed-author:TherienMichelM,
pubmed-author:WilsonMarie-ClaireMC
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pubmed:issnType |
Electronic
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pubmed:day |
1
|
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pubmed:volume |
18
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pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
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pubmed:pagination |
3200-5
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pubmed:meshHeading |
pubmed-meshheading:18477508-Animals,
pubmed-meshheading:18477508-Combinatorial Chemistry Techniques,
pubmed-meshheading:18477508-Diabetes Mellitus,
pubmed-meshheading:18477508-Disease Models, Animal,
pubmed-meshheading:18477508-Drug Design,
pubmed-meshheading:18477508-Drug Screening Assays, Antitumor,
pubmed-meshheading:18477508-Haplorhini,
pubmed-meshheading:18477508-Hydrocarbons, Halogenated,
pubmed-meshheading:18477508-Mice,
pubmed-meshheading:18477508-Molecular Structure,
pubmed-meshheading:18477508-Naphthalenes,
pubmed-meshheading:18477508-Neoplasms,
pubmed-meshheading:18477508-Phosphonic Acids,
pubmed-meshheading:18477508-Protein Tyrosine Phosphatase, Non-Receptor Type 1,
pubmed-meshheading:18477508-Rats
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pubmed:year |
2008
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pubmed:articleTitle |
Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, Merck Frosst Canada Ltd, PO Box 1005, Pointe-Claire-Dorval, Que., Canada. yongxin_han@merck.com
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pubmed:publicationType |
Journal Article
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