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Elsevier, Bioorganic and Medicinal Chemistry Letters, 22(25), p. 5352-5356, 2015

DOI: 10.1016/j.bmcl.2015.09.035

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

Journal article published in 2015 by Daniel W. Kung, David A. Griffith ORCID, William P. Esler, Felix F. Vajdos, Alan M. Mathiowetz, Shawn D. Doran, Paul A. Amor, Scott W. Bagley, Tereece Banks, Shawn Cabral, Kristen Ford, Carmen N. Garcia Irizarry, Margaret S. Landis, Kathrine Loomis, Kirk McPherson and other authors.
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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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 0.30μM.