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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 pharmacokinetic study services.

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.