Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.
Bioorg Med Chem Lett
; 18(6): 1939-44, 2008 Mar 15.
Article
in En
| MEDLINE
| ID: mdl-18291645
ABSTRACT
A novel class of azetidinone acid-derived dual PPARalpha/gamma agonists has been synthesized for the treatment of diabetes and dyslipidemia. The preferred stereochemistry in this series for binding and functional agonist activity against both PPARalpha and PPARgamma receptors was shown to be 3S,4S. Synthesis, in vitro and in vivo activities of compounds in this series are described. A high-yielding method for N-arylation of azetidinone esters is also described.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Azetidines
/
PPAR alpha
/
PPAR gamma
Limits:
Animals
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2008
Document type:
Article
Affiliation country: