2. Academic Validation
  3. Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series

Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series

  • Bioorg Med Chem Lett. 2012 Jan 1;22(1):623-7. doi: 10.1016/j.bmcl.2011.10.070.
Nicolas Lachance 1,  Sébastien Guiral,  Zheng Huang,  Jean-Philippe Leclerc,  Chun Sing Li,  Renata M Oballa,  Yeeman K Ramtohul,  Hao Wang,  Jin Wu,  Lei Zhang
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, 16711 TransCanada Hwy, Kirkland, Quebec, Canada H9H 3L1. nicolas.lachance21@gmail.com
PMID: 22101133 DOI: 10.1016/j.bmcl.2011.10.070
Abstract

Elevated levels of stearoyl-CoA desaturase (SCD) activity have been implicated in metabolic disorders such as obesity and type II diabetes. To circumvent skin and eye adverse events observed in rodents with systemically-distributed inhibitors, our research efforts have been focused on the search for new liver-targeting compounds. This work has led to the discovery of novel, potent and liver-selective acyclic linker SCD inhibitors. These compounds possess suitable cellular activity and pharmacokinetic properties to inhibit liver SCD activity in a mouse pharmacodynamic model.

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