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.
Subject(s)
Antiparasitic Agents/chemical synthesis , Antiparasitic Agents/pharmacology , Benzyl Compounds/chemical synthesis , Benzyl Compounds/pharmacology , Butanes/chemical synthesis , Butanes/pharmacology , Animals , Dose-Response Relationship, Drug , Structure-Activity Relationship , Trichomonas vaginalis/drug effects , Trypanosoma cruzi/drug effectsABSTRACT
New nitro- and aminoquinoline derivatives containing a pyridyl nucleus were synthesized from 6, 8-disubstituted 4-methyl-2-pyridylquinolines, which were prepared from N-pyridylmethylidenanilines. The anti-chagasic and trichomonacidal in vitro activity, as well as the cytotoxic properties towards macrophages of some of these compounds were evaluated. Although some of the compounds showed only moderate activity it was possible to establish some structure-activity relationships.
