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Selective thyroid hormone receptor β agonists with oxadiazolone acid isosteres.

Authors
  • Kirschberg, Thorsten A1
  • Jones, Christopher T2
  • Xu, Yingzi2
  • Fenaux, Martijn2
  • Halcomb, Randall L2
  • Wang, Yujin2
  • Klucher, Kevin2
  • 1 Terns Pharmaceuticals Inc., 1065 E. Hillsdale Blvd., Suite 100, Foster City, CA 94404, USA. Electronic address: [email protected]
  • 2 Terns Pharmaceuticals Inc., 1065 E. Hillsdale Blvd., Suite 100, Foster City, CA 94404, USA.
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Aug 05, 2020
Volume
30
Issue
21
Pages
127465–127465
Identifiers
DOI: 10.1016/j.bmcl.2020.127465
PMID: 32768645
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

Use of the oxadiazolone acid isostere in triiodothyronine analogs yielded potent and selective agonists for the thyroid hormone receptor β. Selected examples showed good in-vivo efficacy in a rat hypercholesterolemic model. One compound was further profiled in a diet-induced mouse model of nonalcoholic steatohepatitis (NASH) and showed robust target engagement and significant histological improvements in both liver steatosis and fibrosis. Copyright © 2020. Published by Elsevier Ltd.

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