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Synthesis of novel bicyclo[4.1.0]heptane and bicyclo[3.1.0]hexane derivatives as melanin-concentrating hormone receptor R1 antagonists |
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| Authors: | Su Jing Tang Haiqun McKittrick Brian A Gu Huizhong Guo Tao Qian Gang Burnett Duane A Clader John W Greenlee William J Hawes Brian E O'neill Kim Spar Brian Weig Blair Kowalski Timothy Sorota Steve |
| Institution: | Department of Chemical Research, Schering-Plough Research Institute K15 2545, Kenilworth, NJ 07033, USA. jing.su@spcorp.com |
| 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. |
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