Synthesis of β-hydroxy-propenamide derivatives and the inhibition of human dihydroorotate dehydrogenase
Novel β-hydroxy propenamides as analogues of the active metabolite of leflunomide (A 771726) were synthesized and evaluated for their inhibitory activity on dihydroorotate dehydrogenase (DHODH) in an investigation into their immunosuppressive activity. Compounds2a, 3a, and3h were approximately 4–40 times more potent than leflunomide in their activity while they wereless active than A 771726.
Key wordsImmunosuppressive activity A 771726 Leflunomide Succinyl acetone β-Hydroxy propenamides Dihydroorotate dehydrogenase (DHODH)
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