title: 2-Arylpaullones are selective antitrypanosomal agents.
abstract: Antileishmanial paullone-chalcone hybrid molecules display antiparasitic activity against Trypanosoma brucei rhodesiense blood stream forms, albeit with low selectivity against human THP-1 cells. In order to develop less toxic analogues, paullones with acrylamide or aryl substituents in 2-position were synthesized, of which the latter exhibited potent antiparasitic activity with excellent selectivity profiles. The most potent compound identified in this study was 9-tert-butyl-2-(4-morpholinophenyl)paullone (3i) which inhibited the parasites at submicromolar concentrations (GI50 = 510 nM) with a selectivity index of 157.
authors: Technische Universität Braunschweig, Institut für Medizinische und Pharmazeutische Chemie, Beethovenstraße 55, D-38106 Braunschweig, Germany.
authors: Jasmin
authors: J
authors: Ryczak
authors: Ma'ayan
authors: M
authors: Papini
authors: Annette
authors: A
authors: Lader
authors: Abedelmajeed
authors: A
authors: Nasereddin
authors: Dmitry
authors: D
authors: Kopelyanskiy
authors: Lutz
authors: L
authors: Preu
authors: Charles L
authors: CL
authors: Jaffe
authors: Conrad
authors: C
authors: Kunick
mesh_terms: D001552:Benzazepines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D016833:Trypanosoma brucei rhodesiense / Q000187:drug effects*
chemical_list: D001552:Benzazepines; D014344:Trypanocidal Agents; C547599:paullone