| Synthesis of iodinated biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors. | |
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MedLine Citation:
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PMID: 11814785 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The discoveries of Sch 48461 and Sch 58235 and their novel pharmacology of inhibition of cholesterol absorption have prompted efforts to determine their biological mechanism of action (MOA). To this end, a series of radioiodinated analogues with good to excellent in vivo activity have been designed and synthesized as single enantiomers. They are structurally consistent with the allowable SAR of the 2-azetidinone class of cholesterol absorption inhibitors. |
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Authors:
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Duane A Burnett; Mary Ann Caplen; Martin S Domalski; Margaret E Browne; Harry R Davis; John W Clader |
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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: 12 ISSN: 0960-894X ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2002 Feb |
Date Detail:
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Created Date: 2002-01-29 Completed Date: 2002-06-18 Revised Date: 2005-11-17 |
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: 311-4 Citation Subset: IM |
Affiliation:
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Schering-Plough Research Institute, 2015 Galloping Hill Road MS 2800, Kenilworth, NJ 07033-0539, USA. duane.burnett@spcorp.com |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Anticholesteremic Agents / chemical synthesis*, pharmacology* Azetidines / chemical synthesis*, chemistry, pharmacology* Cholesterol / pharmacokinetics* Cricetinae Drug Design Intestinal Absorption / drug effects* Isotope Labeling Stereoisomerism Structure-Activity Relationship |
| Chemical | |
Reg. No./Substance:
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0/2-azetidinone; 0/Anticholesteremic Agents; 0/Azetidines; 148260-92-8/1,4-bis(4-methoxyphenyl)-3-(3-phenylpropyl)-2-azetidinone; 163222-33-1/ezetimibe; 57-88-5/Cholesterol |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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