title: 4-nitroacetophenone-derived thiosemicarbazones and their copper(II) complexes with significant in vitro anti-trypanosomal activity.
abstract: N(4)-methyl-4-nitroacetophenone thiosemicarbazone (H4NO(2)Ac4M, 1), N(4),N(4)-dimethyl-4-nitroacetophenone thiosemicarbazone (H4NO(2)Ac4DM, 2) and N(4)-piperidyl-4-nitroacetophenone thiosemicarbazone (H4NO(2)Ac4Pip, 3) and their copper(II) complexes [Cu(4NO(2)Ac4M)(2)] (4), [Cu(4NO(2)Ac4DM)(2)] (5) and [Cu(4NO(2)Ac4Pip)(2)] (6) were tested for their in vitro ability to inhibit the growth of Trypanosoma cruzi epimastigote forms. H4NO(2)Ac4DM (2), [Cu(4NO(2)Ac4M)(2)] (4) and [Cu(4NO(2)Ac4DM)(2)] (5) proved to be as active as the clinical reference drugs nifurtimox and benznidazol. Taking into consideration the serious side effects and the poor efficacy of the reference drugs, as well as the appearance of resistance during treatment, the studied compounds could constitute a new class of anti-trypanosomal drug candidates.
authors: Departamento de Química, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, MG, Brazil.
authors: Anayive
authors: A
authors: Pérez-Rebolledo
authors: Letícia R
authors: LR
authors: Teixeira
authors: Alzir A
authors: AA
authors: Batista
authors: Antonio S
authors: AS
authors: Mangrich
authors: Gabriela
authors: G
authors: Aguirre
authors: Hugo
authors: H
authors: Cerecetto
authors: Mercedes
authors: M
authors: González
authors: Paola
authors: P
authors: Hernández
authors: Ana M
authors: AM
authors: Ferreira
authors: Nivaldo L
authors: NL
authors: Speziali
authors: Heloisa
authors: H
authors: Beraldo
mesh_terms: D000098:Acetophenones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D002614:Chelating Agents / Q000138:chemical synthesis* / Q000737:chemistry; D003300:Copper; D018360:Crystallography, X-Ray; D004563:Electrochemistry; D004578:Electron Spin Resonance Spectroscopy; D006801:Humans; D066298:In Vitro Techniques; D008264:Macrophages / Q000187:drug effects / Q000469:parasitology; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D013882:Thiosemicarbazones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014349:Trypanosoma cruzi / Q000187:drug effects
chemical_list: D000098:Acetophenones; D002614:Chelating Agents; D013882:Thiosemicarbazones; D014344:Trypanocidal Agents; D003300:Copper