Aryloxazolidinediones: Identification of potent orally active PPAR dual α/γ agonists

A series of novel aryloxazolidine-2,4-diones was synthesized. A structure-activity relationship study of these compounds led to the identification of potent, orally active PPAR dual alpha/gamma agonists. Based on the results of efficacy studies in the db/db mice model of type 2 diabetes and the desi...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-10, Vol.13 (20), p.3541-3544
Main Authors: DESAI, Ranjit C, GRATALE, Dominick F, FRANKLIN, Ronald, MOLLER, David E, HECK, James V, SAHOO, Soumya P, WEI HAN, KOYAMA, Hiroo, METZGER, Edward, LOMBARDO, Victoria K, MACNAUL, Karen L, DOEBBER, Thomas W, BERGER, Joel P, LEUNG, Kwan
Format: Article
Language:English
Subjects:
Administration, Oral
Biological and medical sciences
General and cellular metabolism. Vitamins
Hypoglycemic Agents - chemistry
Hypoglycemic Agents - pharmacokinetics
Hypoglycemic Agents - pharmacology
Medical sciences
Oxazoles - chemistry
Oxazoles - pharmacokinetics
Oxazoles - pharmacology
Pharmacology. Drug treatments
Receptors, Cytoplasmic and Nuclear - agonists
Structure-Activity Relationship
Transcription Factors - agonists
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Summary:A series of novel aryloxazolidine-2,4-diones was synthesized. A structure-activity relationship study of these compounds led to the identification of potent, orally active PPAR dual alpha/gamma agonists. Based on the results of efficacy studies in the db/db mice model of type 2 diabetes and the desired pharmacokinetic parameters, compound 12 was selected for further profiling.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(03)00785-6