Synthesis and antiparasitic properties of new 4-N-benzylamino-4-hetarylbut-1-enes

Arch Pharm (Weinheim). 2005 Jan;338(1):32-7. doi: 10.1002/ardp.200400909.

Abstract

New derivatives of 4-N-benzylamino-4-hetarylbut-1-ene containing a pyridyl nucleus were synthesized from benzylamines and pyridine aldehydes. N-oxide derivatives were obtained from these homoallylamines. Study of the antiparasitic properties of obtained pyridine derivatives as well as of four related benzazepines previously described, was carried out using cytotoxicity assays against Trichomonas vaginalis and epimastigote form of Trypanosoma cruzi protozoa. Compounds showing activity against epimastigote T. cruzi were tested against the amastigote form; unspecific cytotoxicity against macrophages was also studied.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiparasitic Agents / chemical synthesis*
  • Antiparasitic Agents / pharmacology*
  • Benzyl Compounds / chemical synthesis*
  • Benzyl Compounds / pharmacology*
  • Butanes / chemical synthesis*
  • Butanes / pharmacology*
  • Dose-Response Relationship, Drug
  • Structure-Activity Relationship
  • Trichomonas vaginalis / drug effects
  • Trypanosoma cruzi / drug effects

Substances

  • Antiparasitic Agents
  • Benzyl Compounds
  • Butanes