Discovery of liver selective non-steroidal glucocorticoid receptor antagonist as novel antidiabetic agents
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- 作者：Kiran Shah ; Dipam Patel ; Pradip Jadav ; Mubeen Sheikh ; Kalapatapu V.V.M. Sairam ; Amit Joharapurkar ; Mukul R. Jain ; Rajesh Bahekar
- 关键词：Glucocorticoid ; Diabetes ; Antagonist ; Non-steroidal ; Liver Selective
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2012
- 出版时间：15 September, 2012
- 年：2012
- 卷：22
- 期：18
- 页码：5857-5862
- 全文大小：669 K
文摘
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.