2. Academic Validation
  3. 1,2,5-Oxadiazole analogues of leflunomide and related compounds

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

Affiliation

  • 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).

Figures
Products