| Discovery of cyclic amine-substituted benzoic acids as PPARα agonists. | |
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MedLine Citation:
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PMID: 22133631 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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A series of novel cyclic amine-substituted benzoic acid derivatives were synthesized and evaluated for their PPARα agonist activity. Strucure-activity relationship studies led to the identification of (S)-3-[3-[2-(4-chlorophenyl)-4-methylthyazole-5-carboxamido]piperidin-1-yl]benzoic acid (S)-4f (KRP-105) as a potent and high subtype-selective human PPARα agonist. (S)-4f showed excellent PK profile and oral administration of (S)-4f to high-fat diet dogs effectively lowered triglycerides. |
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Authors:
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Masahiro Nomura; Kazuhiro Yumoto; Takehiro Shinozaki; Shigeki Isogai; Yasuo Takano; Koji Murakami |
Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-11-9 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: - ISSN: 1464-3405 ISO Abbreviation: - Publication Date: 2011 Nov |
Date Detail:
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Created Date: 2011-12-2 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2011 Elsevier Ltd. All rights reserved. |
Affiliation:
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Discovery Research Laboratories, Kyorin Pharmaceutical Co., Ltd, 2399-1, Nogi, Nogi-machi, Shimotsuga-gun, Tochigi 329-0114, Japan. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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