Document Detail


Design, synthesis, and structure-activity relationships of piperidine and dehydropiperidine carboxylic acids as novel, potent dual PPARalpha/gamma agonists.
MedLine Citation:
PMID:  18511276     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Several series of substituted dehydropiperidine and piperidine-4-carboxylic acid analogs have been designed and synthesized as novel, potent dual PPARalpha/gamma agonists. The SAR of these series of analogs is discussed. A rare double bond migration occurred during the basic hydrolysis of the alpha,beta-unsaturated dehydropiperidine esters 12, and the structures of the migration products were confirmed through a series of 2D NMR experiments.
Authors:
Xiang-Yang Ye; Yi-Xin Li; Dennis Farrelly; Neil Flynn; Liqun Gu; Kenneth T Locke; Jonathan Lippy; Kevin O'Malley; Celeste Twamley; Litao Zhang; Denis E Ryono; Robert Zahler; Narayanan Hariharan; Peter T W Cheng
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Publication Detail:
Type:  Journal Article     Date:  2008-05-06
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  18     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2008 Jun 
Date Detail:
Created Date:  2008-06-10     Completed Date:  2008-08-25     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  3545-50     Citation Subset:  IM    
Affiliation:
Metabolic Diseases Chemistry, Bristol-Myers Squibb R&D, PO Box 5400, Princeton, NJ 08543-5400, USA. xiang-yang.ye@bms.com
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MeSH Terms
Descriptor/Qualifier:
Binding, Competitive / drug effects
Carboxylic Acids* / chemical synthesis,  chemistry,  pharmacology
Dose-Response Relationship, Drug
Drug Design
Humans
Inhibitory Concentration 50
Molecular Structure
PPAR alpha / agonists*
PPAR gamma / agonists*
Piperidines* / chemical synthesis,  chemistry,  pharmacology
Stereoisomerism
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/Carboxylic Acids; 0/PPAR alpha; 0/PPAR gamma; 0/Piperidines

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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