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).

1,2,5-Oxadiazole analogues of leflunomide and related compounds

GIORGIS, Marta;LOLLI, Marco Lucio;ROLANDO, Barbara;TOSCO, Paolo;MARABELLO, Domenica;FRUTTERO, Roberta;GASCO, Alberto
2011

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).
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http://www.elsevier.com/locate/ejmech
Cyano-oximes; Dihydroorotate dehydrogenase inhibitors; Furazans; Leflunomide.
Marta Giorgis; Marco Lucio Lolli; Barbara Rolando; Angela Rao; Paolo Tosco; Shilpi Chaurasia; Domenica Marabello; Roberta Fruttero; Alberto Gasco.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2318/81665
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