Document Detail


Synthesis of iodinated biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors.
MedLine Citation:
PMID:  11814785     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Duane A Burnett; Mary Ann Caplen; Martin S Domalski; Margaret E Browne; Harry R Davis; John W Clader
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  12     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2002 Feb 
Date Detail:
Created Date:  2002-01-29     Completed Date:  2002-06-18     Revised Date:  2005-11-17    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  311-4     Citation Subset:  IM    
Affiliation:
Schering-Plough Research Institute, 2015 Galloping Hill Road MS 2800, Kenilworth, NJ 07033-0539, USA. duane.burnett@spcorp.com
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MeSH Terms
Descriptor/Qualifier:
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:
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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