Conversion of systemically-distributed triazole-based stearoyl-CoA desaturase (SCD) uHTS hits into liver-targeted SCD inhibitors.

Basic Information

ID: ALA1914316

Journal: Bioorg Med Chem Lett

Title: Conversion of systemically-distributed triazole-based stearoyl-CoA desaturase (SCD) uHTS hits into liver-targeted SCD inhibitors.

Authors: Leclerc JP, Falgueyret JP, Girardin M, Guay J, Guiral S, Huang Z, Li CS, Oballa R, Ramtohul YK, Skorey K, Tawa P, Wang H, Zhang L.

Abstract: 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.

CiteXplore: 21924609

DOI: 10.1016/j.bmcl.2011.08.073

Patent ID: ┄