title: Antiprotozoal activity of synthetic amino substituted 1-methyl-1 H-alpha-carbolines.
abstract: The antiprotozoal properties of a series of amino substituted 1-methyl-1 H-alpha-carbolines were investigated in a broad panel of parasites. Various substituents were systematically introduced at various positions on the carbocyclic ring of the parent 1-methyl-1 H-alpha-carboline. Most compounds showed a potent antiprotozoal activity, although mostly accompanied by cytotoxicity on MRC-5 cells. One compound, containing the same amino-substitution as chloroquine, showed an IC50 against Plasmodium falciparum of 2.37 microM and was reasonably selective.
authors.forename: S
authors.initials: S
authors.lastname: Verbeeck
authors.forename: A K
authors.initials: AK
authors.lastname: Yadav
authors.forename: B U W
authors.initials: BU
authors.lastname: Maes
authors.forename: K
authors.initials: K
authors.lastname: Augustyns
authors.forename: P
authors.initials: P
authors.lastname: Van Der Veken
authors.forename: P
authors.initials: P
authors.lastname: Cos
authors.forename: L
authors.initials: L
authors.lastname: Maes
authors.forename: L
authors.initials: L
authors.lastname: Pieters
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology*; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002243:Carbolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D018314:Leishmania infantum / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship; D014346:Trypanosoma brucei brucei / Q000187:drug effects; D014349:Trypanosoma cruzi / Q000187:drug effects
chemical_list: D000962:Antimalarials; D000981:Antiprotozoal Agents; D002243:Carbolines