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Discovery of liver selective non-steroidal glucocorticoid receptor antagonist as novel antidiabetic agents.

Abstract：

:Series of benzyl-phenoxybenzyl amino-phenyl acid derivatives (8a-q) are reported as non-steroidal GR antagonist. Compound 8g showed excellent h-GR binding and potent antagonistic activity (in vitro). The lead compound 8g exhibited significant oral antidiabetic and antihyperlipidemic effects (in vivo), along with liver selectivity. These preliminary results confirm discovery of potent and liver selective passive GR antagonist for the treatment of T2DM.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Shah K,Patel D,Jadav P,Sheikh M,Sairam KV,Joharapurkar A,Jain MR,Bahekar R

doi

10.1016/j.bmcl.2012.07.078

subject

Has Abstract

pub_date

2012-09-15 00:00:00

pages

5857-62

issue

18

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00963-8

journal_volume

22

pub_type

杂志文章

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