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Archives of Pharmacal Research

, Volume 26, Issue 3, pp 197–201 | Cite as

Synthesis of β-hydroxy-propenamide derivatives and the inhibition of human dihydroorotate dehydrogenase

  • Taek Hyeon Kim
  • Hye -Sun Na
  • Monika Löffler
Research Article Articles

Abstract

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 words

Immunosuppressive activity A 771726 Leflunomide Succinyl acetone β-Hydroxy propenamides Dihydroorotate dehydrogenase (DHODH) 

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Copyright information

© The Pharmaceutical Society of Korea 2003

Authors and Affiliations

  • Taek Hyeon Kim
    • 1
  • Hye -Sun Na
    • 1
  • Monika Löffler
    • 2
  1. 1.Department of Applied Chemistry, College of EngineeringChonnam National UniversityGwangjuKorea
  2. 2.Institute for Physiological Chemistry, School of MedicinePhilipps-UniversityMarburgGermany

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