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KMID : 0043320030260030197
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Archives of Pharmacal Research
2003 Volume.26 No. 3 p.197 ~ p.201
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Synthesis of b-Hydroxy-Propenamide Derivatives and the Inhibition of Human Dihydroorotate Dehydrogenase
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Kim Taek-Hyeon
Na Hye-Sun
Monika Loffler
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Abstract
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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.
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