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 relate...

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Bibliographic Details
Published in:Archiv der Pharmazie (Weinheim) 2005-01, Vol.338 (1), p.32-37
Main Authors: Kouznetsov, Vladimir V., Castro, Juliette Rivero, Puentes, Cristian Ochoa, Stashenko, Elena E., Martínez, Jairo René, Ochoa, Carmen, Pereira, David Montero, Ruiz, Juan J. Nogal, Portillo, Carlos Fernández, Serrano, Susana Muelas, Barrio, Alicia Gómez, Bahsas, Alí, Amaro-Luis, Juan
Format: Article
Language:English
Subjects:
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antichagasic
Antiparasitic agents
Antiparasitic Agents - chemical synthesis
Antiparasitic Agents - pharmacology
Benzazepines
Benzyl Compounds - chemical synthesis
Benzyl Compounds - pharmacology
Biological and medical sciences
Butanes - chemical synthesis
Butanes - pharmacology
Dose-Response Relationship, Drug
Homoallylamines
Medical sciences
N-oxides
Pharmacology. Drug treatments
Structure-Activity Relationship
Trichomonacidal properties
Trichomonas vaginalis
Trichomonas vaginalis - drug effects
Trypanosoma cruzi
Trypanosoma cruzi - drug effects
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Summary: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.
ISSN:0365-6233
1521-4184
DOI:10.1002/ardp.200400909