| Substituted imidazoles as glucagon receptor antagonists. | |
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MedLine Citation:
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PMID: 11549467 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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A modestly active, nonselective triarylimidazole lead was optimized for binding affinity with the human glucagon receptor. This led to the identification of a 2- and/or 4-alkyl or alkyloxy substituent on the imidazole C4-aryl group as a structural determinant for significant enhancement in binding with the glucagon receptor (e.g., 41, IC(50)=0.053 microM) and selectivity (>1000x) over p38MAP kinase in this class of compounds. |
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Authors:
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L L Chang; K L Sidler; M A Cascieri; S de Laszlo; G Koch; B Li; M MacCoss; N Mantlo; S O'Keefe; M Pang; A Rolando; W K Hagmann |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 11 ISSN: 0960-894X ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2001 Sep |
Date Detail:
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Created Date: 2001-09-10 Completed Date: 2002-03-12 Revised Date: 2009-11-19 |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 2549-53 Citation Subset: IM |
Affiliation:
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Department of Medicinal Chemical Research, Merck Research Laboratories, Rahway, NJ 07065, USA. linda_chang@merck.com |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals CHO Cells Cricetinae Drug Design Drug Evaluation, Preclinical Humans Imidazoles / chemistry Inhibitory Concentration 50 Magnesium / metabolism, pharmacology Mitogen-Activated Protein Kinases / drug effects, metabolism Pyridines / chemistry*, metabolism, pharmacology* Receptors, Glucagon / antagonists & inhibitors*, metabolism Structure-Activity Relationship p38 Mitogen-Activated Protein Kinases |
| Chemical | |
Reg. No./Substance:
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0/Imidazoles; 0/Pyridines; 0/Receptors, Glucagon; 7439-95-4/Magnesium; EC 2.7.11.24/Mitogen-Activated Protein Kinases; EC 2.7.11.24/p38 Mitogen-Activated Protein Kinases |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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