Synthesis and antiparasitic properties of new 4-N-benzylamino-4-hetarylbut-1-enes.
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.
Kouznetsov
Vladimir V
VV
Laboratory of Fine Organic Synthesis, Research Center for Biomolecules, School of Chemistry, Industrial University of Santander, AA 678, Bucaramanga, Colombia. kouznet@uis.edu.co
Castro
Juliette Rivero
JR
Puentes
Cristian Ochoa
CO
Stashenko
Elena E
EE
Martínez
Jairo René
JR
Ochoa
Carmen
C
Pereira
David Montero
DM
Ruiz
Juan J Nogal
JJ
Portillo
Carlos Fernández
CF
Serrano
Susana Muelas
SM
Barrio
Alicia Gómez
AG
Bahsas
Alí
A
Amaro-Luis
Juan
J
D000818:Animals; D000977:Antiparasitic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001593:Benzyl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D002073:Butanes / Q000138:chemical synthesis* / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D013329:Structure-Activity Relationship; D014246:Trichomonas vaginalis / Q000187:drug effects; D014349:Trypanosoma cruzi / Q000187:drug effects
D000977:Antiparasitic Agents; D001593:Benzyl Compounds; D002073:Butanes