Synthesis, and biological evaluation of new 1,3,4-thiadiazolium-2-phenylamine derivatives against Leishmania amazonensis promastigotes and amastigotes

Eur J Med Chem. 2002 Dec;37(12):979-84. doi: 10.1016/s0223-5234(02)01401-0.

Abstract

1,3,4-thiadiazolium-2-aminide, which is a class of mesoionic compounds, were tested against promastigote and amastigote forms of Leishmania amazonensis. Parasites were assayed with or without the drugs in axenic media, using pentamidine isethionate as a reference drug. The very promising results showed us the most active compounds were the 4'- and 3'-methoxy derivatives against promastigote forms, while the highest activity against the amastigote forms was obtained with the 4'-fluor and 3'-bromo derivatives.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aniline Compounds / chemical synthesis*
  • Aniline Compounds / chemistry
  • Aniline Compounds / pharmacology*
  • Animals
  • Dose-Response Relationship, Drug
  • Drug Design
  • Leishmania braziliensis / drug effects*
  • Leishmania braziliensis / growth & development*
  • Magnetic Resonance Spectroscopy
  • Models, Molecular
  • Molecular Conformation
  • Structure-Activity Relationship

Substances

  • Aniline Compounds