Abstract
A new series of compounds, structurally related to leflunomide, based on the 1,2,5-oxadiazole ring system (furazan) has been synthesised, and their ability to undergo ring scission at physiological pH to afford the corresponding cyano-oximes has been analyzed. The latter, together with the respective nitro derivatives obtained by oxidation, have been characterised as weak inhibitors of rat dihydroorotate dehydrogenase (DHODH).
Copyright © 2010 Elsevier Masson SAS. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Dihydroorotate Dehydrogenase
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / pharmacology
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Humans
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Isoxazoles / chemistry*
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Isoxazoles / pharmacology
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Leflunomide
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Male
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Models, Molecular
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Oxadiazoles / chemistry*
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Oxidoreductases Acting on CH-CH Group Donors / antagonists & inhibitors
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Oxidoreductases Acting on CH-CH Group Donors / chemistry
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Protein Conformation
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Rats
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Rats, Wistar
Substances
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Dihydroorotate Dehydrogenase
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Enzyme Inhibitors
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Isoxazoles
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Oxadiazoles
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Oxidoreductases Acting on CH-CH Group Donors
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Leflunomide