Conversion of systemically-distributed triazole-based stearoyl-CoA desaturase (SCD) uHTS hits into liver-targeted SCD inhibitors
It has been demonstrated that once-a-day dosing of systemically-distributed SCD inhibitors leads to adverse events in eye and skin. Herein, we describe our efforts to convert a novel class of systemically-distributed potent triazole-based uHTS hits into liver-targeted SCD inhibitors as a means to circumvent chronic toxicity.
Leclerc, Jean-Philippe,Falgueyret, Jean-Pierre,Girardin, Mélina,Guay, Jocelyne,Guiral, Sébastien,Huang, Zheng,Li, Chun Sing,Oballa, Renata,Ramtohul, Yeeman K.,Skorey, Kathryn,Tawa, Paul,Wang, Hao,Zhang, Lei
p. 6505 - 6509
(2011/12/04)
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