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Bicyclic heteroaryl inhibitors of stearoyl-CoA desaturase: from systemic to liver-targeting inhibitors |
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| Authors: | Ramtohul Yeeman K Powell David Leclerc Jean-Philippe Leger Serge Oballa Renata Black Cameron Isabel Elise Li Chun Sing Crane Sheldon Robichaud Joel Guay Jocelyne Guiral Sébastien Zhang Lei Huang Zheng |
| Affiliation: | Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, 16711 TransCanada Hwy, Kirkland, Quebec, Canada H9H 3L1. ramtohul@hotmail.com |
| Abstract: | Optimization of a lead thiazole amide MF-152 led to the identification of potent bicyclic heteroaryl SCD1 inhibitors with good mouse pharmacokinetic profiles. In a view to target the liver for efficacy and to avoid SCD1 inhibition in the skin and eyes where adverse effects were previously observed in rodents, representative systemically-distributed SCD1 inhibitors were converted into liver-targeting SCD1 inhibitors. |
| Keywords: | Stearoyl-CoA SCD1 inhibitors Liver-selective inhibitors Mouse liver PD Desaturation index |
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