Optimization and metabolic stabilization of a class of nonsteroidal glucocorticoid modulators.
The optimization of a series of nonsteroidal glucocorticoid modulators is reported. Potent selective GR ligands that have improved metabolic stability were discovered typified by the subnanomolar acid 12 (GR binding IC(50)=0.6 nM).
Link
J T
JT
Metabolic Disease Research, Abbott Laboratories, Dept 4CB, Bldg. AP-10, Rm. L-14, 100 Abbott Park Road, Abott Park, IL 60064-6098, USA. james.link@abbott.com
Sorensen
Bryan K
BK
Patel
Jyoti
J
Arendsen
David
D
Li
Gaoquan
G
Swanson
Susan
S
Nguyen
Bach
B
Emery
Maurice
M
Grynfarb
Marlena
M
Goos-Nilsson
Annika
A
D006801:Humans; D008024:Ligands; D011485:Protein Binding; D011965:Receptors, Glucocorticoid / Q000187:drug effects* / Q000378:metabolism
D008024:Ligands; D011965:Receptors, Glucocorticoid