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

  • Eur J Med Chem. 2011 Jan;46(1):383-92. doi: 10.1016/j.ejmech.2010.10.029.
Marta Giorgis  1 ,  Marco Lucio Lolli ,  Barbara Rolando ,  Angela Rao ,  Paolo Tosco ,  Shilpi Chaurasia ,  Domenica Marabello ,  Roberta Fruttero ,  Alberto Gasco
Affiliations
  • 1. Dipartimento di Scienza e Tecnologia del Farmaco, Università di Torino, Via Pietro Giuria 9, I-10125 Torino, Italy.
PMID: 21109332 DOI: 10.1016/j.ejmech.2010.10.029
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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