| Discovery of a potent and selective free fatty acid receptor 1 (FFA1) agonist with low lipophilicity and high oral bioavailability. | |
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MedLine Citation:
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PMID: 23294321 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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The free fatty acid receptor 1 (FFA1, also known as GPR40) mediates enhancement of glucose-stimulated insulin secretion and is emerging as a new target for the treatment of type 2 diabetes. Several FFA1 agonists are known, but the majority of these suffer from high lipophilicity. We have previously reported the FFA1 agonist 3 (TUG-424). We here describe the continued structure-activity exploration and optimization of this compound series, leading to the discovery of the more potent agonist 40, a compound with low lipophilicity, excellent in vitro metabolic stability and permeability, complete oral bioavailability and appreciable efficacy on glucose tolerance in mice. |
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Authors:
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Elisabeth Christiansen; Maria E Due-Hansen; Christian Urban; Manuel Grundmann; Johannes Schmidt; Steffen V F Hansen; Brian D Hudson; Mohamed Zaibi; Stine B Markussen; Ellen Hagesaether; Graeme Milligan; Michael A Cawthorne; Evi Kostenis; Matthias Kassack; Trond Ulven |
Publication Detail:
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Type: JOURNAL ARTICLE Date: 2013-1-8 |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: - ISSN: 1520-4804 ISO Abbreviation: J. Med. Chem. Publication Date: 2013 Jan |
Date Detail:
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Created Date: 2013-1-8 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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