title: Synthesis, docking, and in vitro activity of thiosemicarbazones, aminoacyl-thiosemicarbazides and acyl-thiazolidones against Trypanosoma cruzi.
abstract: A novel series of thiosemicarbazone and aminoacyl-thiazolidones derivatives were synthesized. Their structure suggests that these compounds could have anti-Trypanosoma cruzi activity. Biological evaluation indicates that some of these compounds are able to inhibit the growth of T. cruzi in concentrations non-cytotoxic to mammalian cells. Docking studies were carried out in order to investigate the binding pattern of these compounds for the T. cruzi cruzain (TCC) protein, and these showed a significant correlation with experimental data.
authors.affiliation: Avaliação e Síntese de Fármacos-LABSINFA, Departamento de Ciências Farmacêuticas, Universidade Federal de Pernambuco, Rua Prof. Artur Sá S/N, Cidade Universitária, 50740-520 Recife, PE, Brazil. acllb2003@yahoo.com.br
authors.forename: Ana Cristina Lima
authors.initials: AC
authors.lastname: Leite
authors.forename: Renata Souza
authors.initials: RS
authors.lastname: de Lima
authors.forename: Diogo Rodrigo de M
authors.initials: DR
authors.lastname: Moreira
authors.forename: Marcos Veríssimo de O
authors.initials: MV
authors.lastname: Cardoso
authors.forename: Ana Carolina
authors.initials: AC
authors.lastname: Gouveia de Brito
authors.forename: Luciene Maria
authors.initials: LM
authors.lastname: Farias Dos Santos
authors.forename: Marcelo Zaldini
authors.initials: MZ
authors.lastname: Hernandes
authors.forename: Alice Costa
authors.initials: AC
authors.lastname: Kiperstok
authors.forename: Ricardo Santana
authors.initials: RS
authors.lastname: de Lima
authors.forename: Milena B P
authors.initials: MB
authors.lastname: Soares
mesh_terms: D000818:Animals; D006860:Hydrogen Bonding; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D051379:Mice; D008807:Mice, Inbred BALB C; D008958:Models, Molecular; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D012663:Semicarbazides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D012680:Sensitivity and Specificity; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013882:Thiosemicarbazones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D014349:Trypanosoma cruzi / Q000187:drug effects*
chemical_list: D012663:Semicarbazides; D013844:Thiazoles; D013882:Thiosemicarbazones; C005151:thiosemicarbazide