title: 4-Aryl(benzyl)amino-4-heteroarylbut-1-enes as building blocks in heterocyclic synthesis. 4. Synthesis of 4, 6-dimethyl-5-nitro(amino)-2-pyridylquinolines and their antiparasitic activities.
abstract: 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.
authors.affiliation: Laboratory of Fine Organic Synthesis, Research Center for Biomolecules, School of Chemistry, Industrial University of Santander, Bucaramanga, Colombia. kouznet@uis.edu.co
authors.forename: Vladimir V
authors.initials: VV
authors.lastname: Kouznetsov
authors.forename: Leonor Y Vargas
authors.initials: LY
authors.lastname: Méndez
authors.forename: Belsy
authors.initials: B
authors.lastname: Tibaduiza
authors.forename: Carmen
authors.initials: C
authors.lastname: Ochoa
authors.forename: David Montero
authors.initials: DM
authors.lastname: Pereira
authors.forename: Juan J Nogal
authors.initials: JJ
authors.lastname: Ruiz
authors.forename: Carlos Fernaéndez
authors.initials: CF
authors.lastname: Portillo
authors.forename: Susana Muelas
authors.initials: SM
authors.lastname: Serrano
authors.forename: Alicia
authors.initials: A
authors.lastname: Gómez Barrio
authors.forename: Alí
authors.initials: A
authors.lastname: Bahsas
authors.forename: Juan
authors.initials: J
authors.lastname: Amaro-Luis
mesh_terms: D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D000814:Aniline Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000994:Antitrichomonal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002082:Butylamines / Q000138:chemical synthesis* / Q000494:pharmacology; D002460:Cell Line; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D008264:Macrophages / Q000187:drug effects / Q000469:parasitology; D008795:Metronidazole / Q000494:pharmacology; D009547:Nifurtimox / Q000494:pharmacology; D009600:Nitroquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014246:Trichomonas vaginalis / Q000187:drug effects; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D014349:Trypanosoma cruzi / Q000187:drug effects
chemical_list: C486635:4-methyl-5-nitro-2-(3-pyridyl)quinoline; C486636:8-isopropyl-4-methyl-5-nitro-2-(3-pyridyl)quinoline; D000634:Aminoquinolines; D000814:Aniline Compounds; D000994:Antitrichomonal Agents; D002082:Butylamines; D006571:Heterocyclic Compounds; D009600:Nitroquinolines; D011725:Pyridines; D014344:Trypanocidal Agents; D008795:Metronidazole; D009547:Nifurtimox