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A series of DHODH inhibitors as potential rheumatoid arthritis (RA) treatment agents are designed and synthesized. The PK study was conducted by Medicilon

2023-07-11

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Human dihydroorotate dehydrogenase (DHODH) is a viable target for the development of therapeutics to treat cancer and immunological diseases. Herein, researchers designed and synthesized a series of acrylamide-based novel DHODH inhibitors as potential rheumatoid arthritis (RA) treatment agents. The most potent compound 54 displays favorable pharmacokinetic (PK) profiles in vivo. The PK study was conducted by using Medicilon's preclinical.

Reference:

Fanxun Zeng, et al. Design, synthesis, molecular modeling, and biological evaluation of acrylamide derivatives as potent inhibitors of human dihydroorotate dehydrogenase for the treatment of rheumatoid arthritis. Acta Pharm Sin B. 2020 Oct 15;11(3):795-809. doi: 10.1016/j.apsb.2020.10.008.

rheumatoid-arthritis pharmacokinetic PK preclinical

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