Consulta: creatorFacets:"Rando,Daniela Gonçales Galasse"
Registros recuperados: 2
Data/hora: 06/06/2024 04:35:12

4-Phenyl-1,3-thiazole-2-amines as scaffolds for new antileishmanial agents
Provedor de dados: 80
Autores: Rodrigues,Carina Agostinho; Santos,Paloma Freire dos; Costa,Marcela Oliveira Legramanti da; Pavani,Thais Fernanda Amorim; Xander,Patrícia; Geraldo,Mariana Marques; Mengarda,Ana; Moraes,Josué de; Rando,Daniela Gonçales Galasse.
Abstract  Background: There is still a need for new alternatives in pharmacological therapy for neglected diseases, as the drugs available show high toxicity and parenteral administration. That is the case for the treatment of leishmaniasis, particularly to the cutaneous clinical form of the disease. In this study, we present the synthesis and biological screening of eight 4-phenyl-1,3-thiazol-2-amines assayed against Leishmania amazonensis. Herein we propose that these compounds are good starting points for the search of new antileishmanial drugs by demonstrating some of the structural aspects which could interfere with the observed activity, as well as suggesting potential macromolecular targets.  Methods: The compounds were easily synthesized by the...
Tipo: Info:eu-repo/semantics/article
Palavras-chave: 2-aminothiazoles; Antikinetoplastids; Antileishmanial; Cutaneous; Target fishing.
Ano: 2018
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1678-91992018000100317

N-Myristoyltransferases as antileishmanial targets: a piggyback approach with benzoheterocyclic analogues
Provedor de dados: 60
Autores: Junqueira,Luis Otávio; Costa,Marcela Oliveira Legramanti da; Rando,Daniela Gonçales Galasse.
Leishmaniasis is one of the neglected diseases that remain in need for pharmacological alternatives. In this context, N-Myristoyltransferases (NMT) arise as interesting targets to explore since they are involved in the co/post-translational processing of peptides which are responsible for host cell invasion. Studies that consider these enzymes as targets point out the potential of benzoheterocyclic compounds as inhibitors of Candida albicans’s N-myristoyltransferase. Here we applied a combination of comparative binding site analysis and molecular docking studies based on a Piggyback approach in the search for new Leishmania major NMT ligands. Our results revealed that NMT enzymes from both pathogens present enough structural similarity to allow...
Tipo: Info:eu-repo/semantics/article
Palavras-chave: N-myristoyltransferase; Leishmaniasis; Benzofuran; Benzothiazole; Molecular docking; Leishmania major.
Ano: 2019
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502019000100562