Bile acid conjugates of a nonsteroidal glucocorticoid receptor modulator.
Bile acid conjugates of a selective nonsteroidal glucocorticoid receptor modulator were prepared and evaluated. Potent GR binding conjugates that showed improved metabolic stability were discovered. However, cellular potency and pharmacokinetics were not substantially improved.
Tu
Noah
N
Metabolic Disease Research, Abbott Laboratories, Dept 4CB, Building AP-10, Rm. L-14, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA.
Link
J T
JT
Sorensen
Bryan K
BK
Emery
Maurice
M
Grynfarb
Marlena
M
Goos-Nilsson
Annika
A
Nguyen
Bach
B
D000818:Animals; D001647:Bile Acids and Salts / Q000737:chemistry* / Q000493:pharmacokinetics; D001682:Biological Availability; D051381:Rats; D017207:Rats, Sprague-Dawley; D011965:Receptors, Glucocorticoid / Q000187:drug effects*
D001647:Bile Acids and Salts; D011965:Receptors, Glucocorticoid