Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 1 de 1
Filter
Add more filters









Database
Language
Publication year range
1.
Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity.
Sznaidman, Marcos L; Haffner, Curt D; Maloney, Patrick R; Fivush, Adam; Chao, Esther; Goreham, Donna; Sierra, Michael L; LeGrumelec, Christelle; Xu, H Eric; Montana, Valerie G; Lambert, Millard H; Willson, Timothy M; Oliver, William R; Sternbach, Daniel D.
Bioorg Med Chem Lett ; 13(9): 1517-21, 2003 May 05.
Article in English | MEDLINE | ID: mdl-12699745

ABSTRACT

We report the synthesis and biological activity of a new series of small molecule agonists of the human Peroxisome Proliferator-Activated Receptor delta (PPARdelta). Several hits were identified from our original libraries containing lipophilic carboxylic acids. Optimization of these hits by structure-guided design led to 7k (GW501516) and 7l (GW0742), which shows an EC(50) of 1.1 nM against PPARdelta with 1000-fold selectivity over the other human subtypes.


Subject(s)
Receptors, Cytoplasmic and Nuclear/agonists , Thiazoles/chemical synthesis , Transcription Factors/agonists , Animals , Cells, Cultured , Combinatorial Chemistry Techniques , Humans , Mice , Radioligand Assay , Structure-Activity Relationship , Thiazoles/chemistry , Thiazoles/pharmacology , Transcriptional Activation
SEND TO:
Email
Export
Print
RSS
XML
SELECTION OF CITATIONS
SEARCH DETAIL