Identification of a series of PPAR-gamma/delta dual agonists via solid-phase parallel synthesis

Authors
Liu, KG Lambert, MH Leesnitzer, LM Oliver, W Ott, RJ Plunket, KD Stuart, LW Brown, PJ Willson, TM Sternbach, DD
Citation
Kg. Liu et al., Identification of a series of PPAR-gamma/delta dual agonists via solid-phase parallel synthesis, BIOORG MED, 11(22), 2001, pp. 2959-2962
Citations number
18
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
22
Year of publication
2001
Pages
2959 - 2962
Database
ISI
SICI code
0960-894X(20011119)11:22<2959:IOASOP>2.0.ZU;2-P
Abstract
We have developed a general solid-phase synthesis for identification of PPA R ligands. Synthesis of a 480-member library led to the identification of a potent PPAR gamma/delta dual agonist 23. Compound 23 showed good plasma ex posure in rats and demonstrated antihyperglycemic and antihyperlipidemic ef ficacy in diabetic fatty Zucker rats. (C) 2001 Elsevier Science Ltd. All ri ghts reserved.