Identification of a subtype selective human PPARα agonist through parallel-array synthesis
PJ Brown, LW Stuart, KP Hurley, MC Lewis… - Bioorganic & medicinal …, 2001 - Elsevier
PJ Brown, LW Stuart, KP Hurley, MC Lewis, DA Winegar, JG Wilson, WO Wilkison, OR Ittoop…
Bioorganic & medicinal chemistry letters, 2001•ElsevierUsing solid-phase, parallel-array synthesis, a series of urea-substituted thioisobutyric acids
was synthesized and assayed for activity on the human PPAR subtypes. GW7647 (3) was
identified as a potent human PPARα agonist with∼ 200-fold selectivity over PPARγ and
PPARδ, and potent lipid-lowering activity in animal models of dyslipidemia. GW7647 (3) will
be a valuable chemical tool for studying the biology of PPARα in human cells and animal
models of disease.
was synthesized and assayed for activity on the human PPAR subtypes. GW7647 (3) was
identified as a potent human PPARα agonist with∼ 200-fold selectivity over PPARγ and
PPARδ, and potent lipid-lowering activity in animal models of dyslipidemia. GW7647 (3) will
be a valuable chemical tool for studying the biology of PPARα in human cells and animal
models of disease.
Using solid-phase, parallel-array synthesis, a series of urea-substituted thioisobutyric acids was synthesized and assayed for activity on the human PPAR subtypes. GW7647 (3) was identified as a potent human PPARα agonist with ∼200-fold selectivity over PPARγ and PPARδ, and potent lipid-lowering activity in animal models of dyslipidemia. GW7647 (3) will be a valuable chemical tool for studying the biology of PPARα in human cells and animal models of disease.
Elsevier