Synthesis and iNOS/nNOS inhibitory activities of new benzoylpyrazoline derivatives Academic Article uri icon


MeSH Major

  • Imaging, Three-Dimensional
  • Neurites


  • A series of new Δ2-pyrazoline derivatives has been synthesized by means of a 1,3-dipolar-cycloaddition reaction. Ethyl 3-(5-methoxy-2-nitrobenzoyl)-Δ2-pyrazoline-5-carboxylate (5a) has been designed for the formation of the benzoylpyrazoline system present in these derivatives. Two synthetic routes have been utilized changing the starting products in the cycloaddition reaction. In both routes, the majority product obtained was only a Δ2-pyrazoline. The intermediate ethyl 1-acyl-3-(2-nitrobenzoyl-5-substituted)-Δ2-pyrazoline-5- carboxylate derivatives have been transformed into the final compounds by means of several chemical treatments. The compounds have been biologically evaluated as inhibitors of nitric oxide synthase (NOS), showing better affinity towards the inducible NOS isoform than versus neuronal NOS. © 2004 Elsevier Ltd. All rights reserved.

publication date

  • April 26, 2004



  • Academic Article


Digital Object Identifier (DOI)

  • 10.1016/j.tet.2004.03.013

Additional Document Info

start page

  • 4051

end page

  • 4069


  • 60


  • 18