Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 25, Issue 22, Pages 5352-5356Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.09.035
Keywords
Spirocycle; Diamine; ACC; Acetyl CoA-carboxylase
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Funding
- Pfizer, Inc.
- U.S. Department of Energy, Office of Science, Office of Basic Energy Sciences [DE-AC02-98CH10886]
- DOE Office of Biological and Environmental Research [E-SC0012704]
- National Institutes of Health - United States [P41GM103473, P41RR012408]
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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 mu M. (C) 2015 Elsevier Ltd. All rights reserved.
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