Discovery of liver selective non-steroidal glucocorticoid receptor antagonist as novel antidiabetic agents |
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| Authors: | Kiran Shah Dipam Patel Pradip Jadav Mubeen Sheikh Kalapatapu V V M Sairam Amit Joharapurkar Mukul R Jain Rajesh Bahekar |
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| Institution: | Zydus Research Centre, Sarkhej-Bavla N.H. 8A Moraiya, Ahmedabad 382210, India; Department of Chemistry, Faculty of Science, M.S. University of Baroda, Vadodara 380002, India. |
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| 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. |
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