Document Detail

Ezetimibe and other azetidinone cholesterol absorption inhibitors.
MedLine Citation:
PMID:  15857308     Owner:  NLM     Status:  MEDLINE    
Atherosclerotic coronary artery disease remains a major healthcare concern especially in developed countries. While lowering plasma cholesterol levels via diet, exercise, and pharmacotherapy can reduce this risk of developing coronary artery disease, there remains a need for more effective drug therapies. The azetidinone cholesterol absorption inhibitors typified by ezetimibe represent the first new approach to lipid lowering therapy in more than a decade. This review summarizes the medicinal chemistry of the azetidinone cholesterol absorption inhibitors as a class, with emphasis on factors that contributed both to the discovery of ezetimibe as well as to our overall understanding of S.A.R. trends in this area.
John W Clader
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  Current topics in medicinal chemistry     Volume:  5     ISSN:  1568-0266     ISO Abbreviation:  Curr Top Med Chem     Publication Date:  2005  
Date Detail:
Created Date:  2005-04-28     Completed Date:  2005-06-17     Revised Date:  2005-11-16    
Medline Journal Info:
Nlm Unique ID:  101119673     Medline TA:  Curr Top Med Chem     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  243-56     Citation Subset:  IM    
Department of Cardiovascular and CNS Medicinal Chemistry, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033-1300, USA.
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MeSH Terms
Anticholesteremic Agents / pharmacology*,  therapeutic use
Azetidines / pharmacology*,  therapeutic use
Cholesterol / blood*,  metabolism
Coronary Disease / etiology,  mortality,  prevention & control
Drug Therapy, Combination
Intestinal Absorption / drug effects*
Structure-Activity Relationship
Reg. No./Substance:
0/Anticholesteremic Agents; 0/Azetidines; 163222-33-1/ezetimibe; 57-88-5/Cholesterol

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