444341-80-4Relevant articles and documents
Novel 2,3-dihydrobenzofuran-2-carboxylic acids: Highly potent and subtype-selective PPARα agonists with potent hypolipidemic activity
Shi, Guo Q.,Dropinski, James F.,Zhang, Yong,Santini, Conrad,Sahoo, Soumya P.,Berger, Joel P.,MacNaul, Karen L.,Zhou, Gaochao,Agrawal, Arun,Alvaro, Raul,Cai, Tian-Quan,Hernandez, Melba,Wright, Samuel D.,Moller, David E.,Heck, James V.,Meinke, Peter T.
, p. 5589 - 5599 (2007/10/03)
The design and synthesis of a novel class of 2,3-dihydrobenzofuran-2- carboxylic acids as highly potent and subtype-selective PPARα agonists are reported. Systematic study of structure-activity relationships has identified several key structural elements within this class for maintaining the potency and subtype selectivity. Select compounds were evaluated in animal models of dyslipidemia using Syrian hamsters and male Beagle dogs, and all these compounds displayed excellent cholesterol- and triglyceride-lowering activity at dose levels that were much lower than the marketed weak PPARα agonist fenofibrate.
(2R)-2-Methylchromane-2-carboxylic acids: Discovery of selective PPARα agonists as hypolipidemic agents
Koyama, Hiroo,Boueres, Julia K.,Miller, Daniel J.,Berger, Joel P.,MacNaul, Karen L.,Wang, Pei-Ran,Ippolito, Marc C.,Wright, Samuel D.,Agrawal, Arun K.,Moller, David E.,Sahoo, Soumya P.
, p. 3347 - 3351 (2007/10/03)
A SAR study was conducted on chromane-2-carboxylic acid toward selective PPARα agonisim. As a result, highly potent, and selective PPARα agonists were discovered. The optimized compound 43 exhibited robust lowering of total cholesterol levels in hamster and dog animal models.
Benzopyrancarboxylic acid derivatives for the treatment of diabetes and lipid disorders
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, (2008/06/13)
A class of benzopyrancarboxylic acid derivatives comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, d