title: Thiosemicarbazones derived from 1-indanones as new anti-Trypanosoma cruzi agents.
abstract: In the present work, we synthesized a series of thiosemicarbazones derived from 1-indanones with good anti-Trypanosoma cruzi activity. Most of them displayed remarkable trypanosomicidal activity. All the compounds showed nonspecific cytotoxicity on human erythrocytes. The ability of the new compounds to inhibit cruzipain, the major cysteine protease of T. cruzi, was also explored. Thiosemicarbazones 12 and 24 inhibited this enzyme at the dose assayed. This interaction was also studied in terms of molecular docking.
authors: Química Medicinal, Departamento de Farmacología, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Junín, Ciudad Autónoma de Buenos Aires, Argentina.
authors: María E
authors: ME
authors: Caputto
authors: Lucas E
authors: LE
authors: Fabian
authors: Diego
authors: D
authors: Benítez
authors: Alicia
authors: A
authors: Merlino
authors: Natalia
authors: N
authors: Ríos
authors: Hugo
authors: H
authors: Cerecetto
authors: Graciela Y
authors: GY
authors: Moltrasio
authors: Albertina G
authors: AG
authors: Moglioni
authors: Mercedes
authors: M
authors: González
authors: Liliana M
authors: LM
authors: Finkielsztein
mesh_terms: D003546:Cysteine Endopeptidases / Q000378:metabolism; D015853:Cysteine Proteinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D004912:Erythrocytes / Q000187:drug effects; D006801:Humans; D007189:Indans / Q000737:chemistry* / Q000494:pharmacology*; D008958:Models, Molecular; D008968:Molecular Conformation; D015800:Protozoan Proteins; D013882:Thiosemicarbazones / Q000737:chemistry* / Q000494:pharmacology*; D014344:Trypanocidal Agents / Q000737:chemistry* / Q000494:pharmacology; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000201:enzymology
chemical_list: D015853:Cysteine Proteinase Inhibitors; D007189:Indans; D015800:Protozoan Proteins; D013882:Thiosemicarbazones; D014344:Trypanocidal Agents; D003546:Cysteine Endopeptidases; C063214:cruzipain