✦ LIBER ✦
Leflunomide's Bioactive Metabolite Has the Minimal Structural Requirements for the Efficient Inhibition of Human Dihydroorotate Dehydrogenase
✍ Scribed by Christos Papageorgiou; M. Zurini; Hans-Peter Weber; Xaver Borer
- Publisher
- Elsevier Science
- Year
- 1997
- Tongue
- English
- Weight
- 192 KB
- Volume
- 25
- Category
- Article
- ISSN
- 0045-2068
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✦ Synopsis
The Ͱ-cyano-ͱ-hydroxy enamide 1 is an inhibitor of human dihydroorotate dehydrogenase (IC 50 ϭ 0.26 ȐM), the rate-limiting enzyme in the de novo pyrimidine biosynthesis. A structure-activity analysis based on selected derivatives of 1 demonstrates that both its structural characteristics and its physicochemical properties are mandatory for the efficient inhibition of the enzyme.