Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2014 Mar 1;24(5):1437-41.
doi: 10.1016/j.bmcl.2013.12.075. Epub 2013 Dec 27.

4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable stearoyl-CoA desaturase-1 (SCD1) inhibitors: part 2. Pyridazine-based analogs

Shyh-Ming Yang  1 , Yuting Tang  2 , Thomas Rano  2 , Huajun Lu  2 , Gee-Hong Kuo  2 , Michael D Gaul  2 , Yaxin Li  2 , George Ho  2 , Wensheng Lang  2 , James G Conway  2 , Yin Liang  2 , James M Lenhard  2 , Keith T Demarest  2 , William V Murray  2
Affiliations

4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable stearoyl-CoA desaturase-1 (SCD1) inhibitors: part 2. Pyridazine-based analogs

Shyh-Ming Yang et al. Bioorg Med Chem Lett. .

Abstract

Design, synthesis, and biological evaluation of pyridazine-based, 4-bicyclic heteroaryl-piperidine derivatives as potent stearoyl-CoA desaturase-1 (SCD1) inhibitors are described. In a chronic study of selected analog (3e) in Zucker fa/fa (ZF) rat, dose-dependent decrease of body weight gain and plasma fatty acid desaturation index (DI) in both C16 and C18 are also demonstrated. The results indicate that the plasma fatty acid DI may serve as an indicator for direct target engagement and biomarker for SCD1 inhibition.

Keywords: Desaturation index; SCD1 inhibitors; Stearoyl-CoA desaturase; obesity.

PubMed Disclaimer

MeSH terms

LinkOut - more resources