Design, synthesis, and biological evaluation of potent PPARα/δ dual agonists for the treatment of nonalcoholic steatohepatitis. The PK studies, hERG studies, and Ames tests were conducted by Medicilon

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Design, synthesis, and biological evaluation of potent PPARα/δ dual agonists for the treatment of nonalcoholic steatohepatitis. The PK studies, hERG studies, and Ames tests were conducted by Medicilon

2023-07-11

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Nonalcoholic steatohepatitis (NASH) is the advanced subtype of nonalcoholic fatty liver disease (NAFLD) and is becoming a severe global public health problem. PPARα/δ are regarded as potential therapeutic targets for NASH. Herein, researchers report a series of novel triazolone derivatives as PPARα/δ dual agonists.

The pharmacokinetic studies were conducted by Medicilon.

The hERG channel inhibition studies were conducted by Medicilon.

The Ames tests were conducted by Medicilon.

Reference:

Zhiqi Feng, et al. Design, Synthesis, and Biological Evaluation of Triazolone Derivatives as Potent PPARα/δ Dual Agonists for the Treatment of Nonalcoholic Steatohepatitis. J Med Chem. 2022 Feb 10;65(3):2571-2592. doi: 10.1021/acs.jmedchem.1c02002.