当前位置： SCI文献检索 > JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Improving the pharmacokinetic and CYP inhibition profiles of azaxanthene-based glucocorticoid receptor modulators-identification of (S)-5-(2-(9-fluoro-2-(4-(2-hydroxypropan-2-yl)phenyl)-5H-chromeno[2,3-b]pyridin-5-yl)-2-methylpropanamido)-N-(tetrahydro-2H

Improving the pharmacokinetic and CYP inhibition profiles of azaxanthene-based glucocorticoid receptor modulators-identification of (S)-5-(2-(9-fluoro-2-(4-(2-hydroxypropan-2-yl)phenyl)-5H-chromeno[2,3-b]pyridin-5-yl)-2-methylpropanamido)-N-(tetrahydro-2H

Abstract：

:An empirical approach to improve the microsomal stability and CYP inhibition profile of lead compounds 1a and 1b led to the identification of 5 (BMS-341) as a dissociated glucocorticoid receptor modulator. Compound 5 showed significant improvements in pharmacokinetic properties and, unlike compounds 1a-b, displayed a linear, dose-dependent pharmacokinetic profile in rats. When tested in a chronic model of adjuvant-induced arthritis in rat, the ED50 of 5 (0.9 mg/kg) was superior to that of both 1a and 1b (8 and 17 mg/kg, respectively).

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Yang MG,Dhar TG,Xiao Z,Xiao HY,Duan JJ,Jiang B,Galella MA,Cunningham M,Wang J,Habte S,Shuster D,McIntyre KW,Carman J,Holloway DA,Somerville JE,Nadler SG,Salter-Cid L,Barrish JC,Weinstein DS

doi

10.1021/acs.jmedchem.5b00257

subject

Has Abstract

pub_date

2015-05-28 00:00:00

pages

4278-90

issue

10

eissn

0022-2623

issn

1520-4804

journal_volume

58

pub_type

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