Leflunomide's Bioactive Metabolite Has the Minimal Structural Requirements for the Efficient Inhibition of Human Dihydroorotate Dehydrogenase

Autor:	Christos Papageorgiou, M. Zurini, Hans Peter Weber, Xaver Borer
Rok vydání:	1997
Předmět:	chemistry.chemical_classification Chemistry Stereochemistry Organic Chemistry Biochemistry Enzyme Bioactive metabolite Drug Discovery Pyrimidine metabolism Dihydroorotate dehydrogenase medicine Molecular Biology Leflunomide medicine.drug
Zdroj:	Bioorganic Chemistry. 25:233-238
ISSN:	0045-2068
DOI:	10.1006/bioo.1997.1072
Popis:	The α-cyano-β-hydroxy enamide 1 is an inhibitor of human dihydroorotate dehydrogenase (IC 50 = 0.26 μM), 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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::08671e5e1194fb4eeafeb24cd30d1df6 https://doi.org/10.1006/bioo.1997.1072 Zobrazit plný text záznamu Full Text from ScienceDirect