| 2-Arylbenzoxazoles as CETP inhibitors: substitution and modification of the alpha-alkoxyamide moiety. | |
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MedLine Citation:
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PMID: 20036121 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The development of a series of 2-arylbenzoxazole alpha-alkoxyamide and beta-alkoxyamine inhibitors of cholesteryl ester transfer protein (CETP) is described. Highly fluorinated alpha-alkoxyamides proved to be potent inhibitors of CETP in vitro, and the highly fluorinated 2-arylbenzoxazole beta-alkoxyamine 4 showed a desirable combination of in vitro potency (IC(50)=151 nM) and oral bioavailability in the mouse. |
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Authors:
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Julianne A Hunt; Silvia Gonzalez; Florida Kallashi; Milton L Hammond; James V Pivnichny; Xinchun Tong; Suoyu S Xu; Matt S Anderson; Ying Chen; Suzanne S Eveland; Qiu Guo; Sheryl A Hyland; Denise P Milot; Carl P Sparrow; Samuel D Wright; Peter J Sinclair |
Publication Detail:
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Type: Comparative Study; Journal Article Date: 2009-12-16 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 20 ISSN: 1464-3405 ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2010 Feb |
Date Detail:
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Created Date: 2010-02-03 Completed Date: 2010-09-20 Revised Date: - |
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: 1019-22 Citation Subset: IM |
Copyright Information:
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Copyright (c) 2009 Elsevier Ltd. All rights reserved. |
Affiliation:
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Merck Research Laboratories, Rahway, NJ 07065, United States. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Alcohols
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chemical synthesis,
metabolism Amides / chemical synthesis, metabolism Benzoxazoles / chemical synthesis*, metabolism* Cholesterol Ester Transfer Proteins / antagonists & inhibitors*, metabolism* |
| Chemical | |
Reg. No./Substance:
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0/Alcohols; 0/Amides; 0/Benzoxazoles; 0/CETP protein, human; 0/Cholesterol Ester Transfer Proteins; 0/alkoxyl radical |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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