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
. 2015 Nov 15;25(22):5352-6.
doi: 10.1016/j.bmcl.2015.09.035. Epub 2015 Sep 15.

Discovery of spirocyclic-diamine inhibitors of mammalian acetyl CoA-carboxylase

Daniel W Kung  1 , David A Griffith  2 , William P Esler  3 , Felix F Vajdos  4 , Alan M Mathiowetz  5 , Shawn D Doran  6 , Paul A Amor  3 , Scott W Bagley  7 , Tereece Banks  7 , Shawn Cabral  7 , Kristen Ford  8 , Carmen N Garcia-Irizarry  7 , Margaret S Landis  9 , Kathrine Loomis  10 , Kirk McPherson  10 , Mark Niosi  6 , Kristin L Rockwell  8 , Colin Rose  7 , Aaron C Smith  7 , James A Southers  7 , Susan Tapley  10 , Meihua Tu  5 , James J Valentine  8
Affiliations

Discovery of spirocyclic-diamine inhibitors of mammalian acetyl CoA-carboxylase

Daniel W Kung et al. Bioorg Med Chem Lett. .

Abstract

A novel series of spirocyclic-diamine based, isoform non-selective inhibitors of acetyl-CoA carboxylase (ACC) is described. These spirodiamine derivatives were discovered by design of a library to mimic the structural rigidity and hydrogen-bonding pattern observed in the co-crystal structure of spirochromanone inhibitor I. The lead compound 3.5.1 inhibited de novo lipogenesis in rat hepatocytes, with an IC50 of 0.30 μM.

Keywords: ACC; Acetyl CoA-carboxylase; Diamine; Spirocycle.

PubMed Disclaimer

Publication types

LinkOut - more resources