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The Pharmaceutical Society of Korea (대한약학회)
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Synthesis of $\beta$-Hydroxy-Propenamide Derivatives and the Inhibition of Human Dihydroorotate Dehydrogenase

  • Kim, Taek-Hyeon (Department of Applied Chemistry, College of Engineering, Chonnam National University) ;
  • Na, Hye-Sun (Department of Applied Chemistry, College of Engineering, Chonnam National University) ;
  • Loffler, Monika (Institute for Physiological Chemistry, School of Medicine, Philipps-University)
  • Published : 2003.03.01
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Abstract

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.

Keywords

References

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