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Synthesis of BMS-309403-Related Compounds, Including [(14)C]BMS-309403, a Radioligand for Adipocyte Fatty Acid Binding Protein.
MedLine Citation:
PMID:  22223390     Owner:  NLM     Status:  In-Data-Review    
Abstract/OtherAbstract:
Adipocyte fatty acid binding protein (A-FABP; FABP4), which is predominantly expressed in macrophages and adipose tissue, regulates fatty acid storage and lipolysis, and is also an important mediator of inflammation. Here, we report a synthesis of (14)C-labeled 2-[2'-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)biphenyl-3-yloxy]acetic acid (BMS309403), a potent and selective small-molecular FABP4 inhibitor, as a chemical tool for investigating the roles of FABP4 in inflammatory and metabolic disorders. The structure-activity relationship of several BMS derivatives for inhibition of FABP4 is also reported.
Authors:
Toshihiko Okada; Makoto Hiromura; Masato Otsuka; Shuichi Enomoto; Hiroyuki Miyachi
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Chemical & pharmaceutical bulletin     Volume:  60     ISSN:  1347-5223     ISO Abbreviation:  Chem. Pharm. Bull.     Publication Date:  2012  
Date Detail:
Created Date:  2012-01-06     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0377775     Medline TA:  Chem Pharm Bull (Tokyo)     Country:  Japan    
Other Details:
Languages:  eng     Pagination:  164-8     Citation Subset:  IM    
Affiliation:
Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University.
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