1.
Nucleosides Nucleotides Nucleic Acids
; 23(12): 1875-87, 2004.
Article
in English
| MEDLINE
| ID: mdl-15628746
ABSTRACT
A new synthesis of (-)-DAPD, suitable for large scale development, is described.
Subject(s)
Antiviral Agents/chemical synthesis , Dioxolanes/chemical synthesis , Purine Nucleosides/chemical synthesis , Nucleic Acid Conformation , Stereoisomerism
2.
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
3.
Nucleosides Nucleotides Nucleic Acids
; 21(2): 155-63, 2002.
Article
in English
| MEDLINE
| ID: mdl-11991142
ABSTRACT
A new synthesis of 2'-deoxy-2'-fluoro-5-methyl-beta-L-arabinofuranosyl uracil (13, L-FMAU) was achieved in 10 steps from L-arabinose.
