Author/Authors :
Jing Su، نويسنده , , Haiqun Tang، نويسنده , , Brian A. McKittrick، نويسنده , , Huizhong Gu، نويسنده , , Tao Guo، نويسنده , , Gang Qian، نويسنده , , Duane A. Burnett، نويسنده , , John W. Clader، نويسنده , , William J. Greenlee، نويسنده , , Brian E. Hawes، نويسنده , , Kim O’Neill، نويسنده , , Brian Spar، نويسنده , , Blair Weig، نويسنده , , Timothy Kowalski، نويسنده , , Steve Sorota، نويسنده ,
Abstract :
To address the hERG liability of MCHR1 antagonists such as 1 and 2, new analogs such as 4 and 5 that incorporated a polar heteroaryl group were designed and synthesized. Biological evaluation confirmed that these new analogs retained MCH R1 activity with greatly attenuated hERG liabilities as indicated in the Rb efflux assay.
