Synthesis and GABA receptor potency of 3-thiomethyl-4-(hetero)aryl-5-amino-1-phenylpyrazoles

Bioorg Med Chem Lett. 2004 Oct 4;14(19):4949-53. doi: 10.1016/j.bmcl.2004.07.033.

Abstract

A convenient synthetic route to novel 4-arylpyrazoles is described. The potential for insecticidal activity through GABA channel blockage by this series of compounds, as well as their selectivity for insect versus mammalian receptors, are explored through in vitro and in vivo assays.

MeSH terms

  • Animals
  • Houseflies
  • Insecticides / chemical synthesis*
  • Insecticides / pharmacology
  • Mice
  • Pyrazoles / chemical synthesis*
  • Pyrazoles / metabolism
  • Pyrazoles / pharmacology
  • Receptors, GABA / drug effects*
  • Receptors, GABA / metabolism
  • Structure-Activity Relationship

Substances

  • Insecticides
  • Pyrazoles
  • Receptors, GABA