1098176-66-9Relevant academic research and scientific papers
Synthetic compounds from an in house library as inhibitors of falcipain-2 from Plasmodium falciparum
Bertoldo, Jean Borges,Chiaradia-Delatorre, Louise Domeneghini,Mascarello, Alessandra,Leal, Paulo César,Cordeiro, Marlon Norberto Sechini,Nunes, Ricardo José,Sarduy, Emir Salas,Rosenthal, Philip Jon,Terenzi, Hernán
, p. 299 - 307 (2015)
Falcipain-2 (FP-2) is a key cysteine protease from the malaria parasite Plasmodium falciparum. Many previous studies have identified FP-2 inhibitors; however, none has yet met the criteria for an antimalarial drug candidate. In this work, we assayed an in-house library of non-peptidic organic compounds, including (E)-chalcones, (E)-N'-benzylidene-benzohydrazides and alkyl-esters of gallic acid, and assessed the activity toward FP-2 and their mechanisms of inhibition. The (E)-chalcones 48, 54 and 66 showed the lowest IC50 values (8.5±0.8μM, 9.5±0.2μM and 4.9±1.3μM, respectively). The best inhibitor (compound 66) demonstrated non-competitive inhibition, and using mass spectrometry and fluorescence spectroscopy assays, we suggest a potential allosteric site for the interaction of this compound, located between the catalytic site and the hemoglobin binding arm in FP-2. We combined structural biology tools and mass spectrometry to characterize the inhibition mechanisms of novel compounds targeting FP-2.
Synthesis and evaluation of new chalcones, derived pyrazoline and cyclohexenone derivatives as potent antimicrobial, antitubercular and antileishmanial agents
Monga, Vikramdeep,Goyal, Kamya,Steindel, Mario,Malhotra, Manav,Rajani, Dhanji P.,Rajani, Smita D.
, p. 2019 - 2032 (2014/05/06)
A series of chalcones (1-8) were prepared by Claisen-Schmidt condensation of 3-nitroacetophenone with various aldehydes. These chalcones on cyclization with hydrazine hydrate in the presence of glacial acetic acid, hydrazine hydrate in absolute ethanol an
Antihyperglycemic activity of naphthylchalcones
Damazio, Rosangela Guollo,Zanatta, Ana Paula,Cazarolli, Luisa Helena,Chiaradia, Louise Domeneghini,Mascarello, Alessandra,Nunes, Ricardo José,Yunes, Rosendo Augusto,Barreto Silva, Fátima Regina Mena
experimental part, p. 1332 - 1337 (2010/06/16)
The purpose of the present work was to investigate, following previous works, naphthylchalcones as antihyperglycemic agent in glucose loaded animal model, insulin secretion as well as the action of these compounds on glucose uptake in a target tissue of insulin. The naphthylchalcones were found to have an acute serum glucose-lowering effect in hyperglycemic normal rats. In addition, chalcones 2 and 4 stimulated significantly the insulin secretion induced by glucose. These results suggest that the presence of nitro group and their position in the phenyl rings are responsible for the antihyperglycemic activity of chalcones. Additionally, the effect of chalcones on serum glucose-lowering seems to be a consequence of insulin secretion and these chalcones represent potential compounds with strong antihyperglycemic properties.
Synthetic chalcones as efficient inhibitors of Mycobacterium tuberculosis protein tyrosine phosphatase PtpA
Chiaradia, Louise Domeneghini,Mascarello, Alessandra,Purificacao, Marcela,Vernal, Javier,Cordeiro, Marlon Norberto Sechini,Zenteno, Maria Emilia,Villarino, Andrea,Nunes, Ricardo Jose,Yunes, Rosendo Augusto,Terenzi, Hernan
supporting information; experimental part, p. 6227 - 6230 (2009/06/30)
In the search for lead compounds for new drugs for tuberculosis, the activity of 38 synthetic chalcones were assayed for their potential inhibitory action towards a protein tyrosine phosphatase from Mycobacterium tuberculosis - PtpA. The compounds were ob
