Kim Taek Hyeon, Na Hye-Sun, Löffler Monika
Department of Applied Chemistry, College of Engineering, Chonnam National University, Gwangju 500-757, Korea.
Arch Pharm Res. 2003 Mar;26(3):197-201. doi: 10.1007/BF02976829.
Novel beta-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. Compounds 2a, 3a, and 3h were approximately 4-40 times more potent than leflunomide in their activity while they were-less active than A 771726.
合成了新型β-羟基丙烯酰胺作为来氟米特活性代谢物（A 771726）的类似物，并在对其免疫抑制活性的研究中评估了它们对二氢乳清酸脱氢酶（DHODH）的抑制活性。化合物2a、3a和3h的活性比来氟米特强约4至40倍，但其活性低于A 771726。
