Selective thyroid hormone receptor β agonists with oxadiazolone acid isosteres.
Terns Pharmaceuticals Inc., 1065 E. Hillsdale Blvd., Suite 100, Foster City, CA 94404, USA. Electronic address: [email protected]
Terns Pharmaceuticals Inc., 1065 E. Hillsdale Blvd., Suite 100, Foster City, CA 94404, USA.
- Published Article
Bioorganic & medicinal chemistry letters
- Publication Date
Aug 05, 2020
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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This record was last updated on 10/16/2020 and may not reflect the most current and accurate biomedical/scientific data available from NLM.
The corresponding record at NLM can be accessed at https://www.ncbi.nlm.nih.gov/pubmed/32768645