1322044-06-3Relevant academic research and scientific papers
In vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agents
Fonseca-Berzal, Cristina,Rojas Ruiz, Fernando A.,Escario, José A.,Kouznetsov, Vladimir V.,Gómez-Barrio, Alicia
, p. 1209 - 1213 (2014/03/21)
In this study, a series of 22 pre-synthesized 7-chloro-4-amino(oxy) quinoline derivatives was assayed in vitro as potential antichagasic agents. A primary screening against Trypanosoma cruzi epimastigotes and a non-specific cytotoxicity assay on murine fibroblasts were simultaneously performed, resulting quinolines 3, 7 and 12 with great selectivity (SI) on the extracellular parasite (SI7, SI3, SI12 and SIBZ >9.44). Therefore, the activity of these derivatives was evaluated on intracellular amastigotes, achieving derivative 7 the best SI (SI = 12.73). These results, supported by the in silico prediction of a good oral bioavailability and a suitable risk profile, propose the 4-amino-7- chloroquinoline scaffold as a potential template for designing trypanocidal prototypes.
Synthesis and antimalarial activity of new heterocyclic hybrids based on chloroquine and thiazolidinone scaffolds
Rojas Ruiz, Fernando A.,Garcia-Sanchez, Rory N.,Estupinan, Santiago Villabona,Gomez-Barrio, Alicia,Torres Amado, Diego F.,Perez-Solorzano, Berta Martin,Nogal-Ruiz, Juan J.,Martinez-Fernandez, Antonio R.,Kouznetsov, Vladimir V.
, p. 4562 - 4573 (2011/09/19)
A series of new 21 chloroquine heterocyclic hybrids containing either benzylamino fragment or N-(aminoalkyl)thiazolidin-4-one moiety were synthesized and screened for their antimalarial activity against chloroquine (CQ)-sensitive 3D7 and multidrug-resistance Dd2 strains of Plasmodium falciparum. Although no compounds more active than CQ against 3D7 was found; against Dd2 strain, six compounds, four of them with benzylamino fragment, showed an excellent activity, up to 3-fold more active than CQ. Non specific cytotoxicity on J774 macrophages was observed in some compounds whereas only two of them showed liver toxicity on HepG2 cells. In addition, all active compounds inhibited the ferriprotoporphyrin IX biocrystalization process in concentrations around to CQ. In vivo preliminary results have shown that at least two compounds are as active as CQ against Plasmodium berghei ANKA.
