106663-71-2Relevant academic research and scientific papers
Synthesis of new alkylated and methoxylated analogues of ebselen with antiviral and antimicrobial properties
Pi?tka-Ottlik, Magdalena,Burda-Grabowska, Ma?gorzata,Wo?na, Marta,Waleńska, Joanna,Kaleta, Rafa?,Zaczyńska, Ewa,Piasecki, Egbert,Giurg, Miros?aw
, p. 546 - 556 (2021/02/09)
A series of new mono and disubstituted alkylated and methoxylated benzisoselanzol-3(2H)-ones and bis(2carbamoylaryl)diselenides were prepared in yields ranging from 55% to 95% starting from anthranilic acid and were evaluated for antiviral and antimicrobial activity. The compounds exhibited antiviral activity against Human herpes virus 1 and Encephalomyocarditis virus as well as antimicrobial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Candida albicans. R1 O O R1 COOH N N R2 H Se R2 NH2 Se 2 R1, R2 = Me, OMe, Cl, t-Bu, H.
Water-dependent synthesis of biologically active diaryl diselenides
Pacu?a, Agata J.,Obieziurska, Magdalena,?cianowski, Jacek,Kaczor, Katarzyna B.,Antosiewicz, J?drzej
, p. 153 - 164 (2018/07/05)
A new one-step method for the synthesis of diaryl diselenides has been developed. The reaction of o-iodobenzamides with dilithium diselenide can be controlled by the presence of water providing a simple and efficient protocol to obtain benzisoselenazolones or diaryl diselenides. A series of N-Aryl ebselen derivatives and the corresponding diselenides was obtained. All synthesized compounds were tested in vitro as antioxidants and cytotoxic agents. N-(2,3,4-Trimethoxyphenyl)benzisoselenazol-3(2H)-one was the best in vitro antioxidant and the corresponding diselenide the most potent cytotoxic agent against prostate cancer cell line DU145, being inactive towards healthy prostate cell line PNT1A. Formula parented.
Reaction of bis[(2-chlorocarbonyl)phenyl] diselenide with phenols, aminophenols, and other amines towards diphenyl diselenides with antimicrobial and antiviral properties ?
Giurg, Miros?aw,Go?ab, Anna,Suchodolski, Jakub,Kaleta, Rafa?,Krasowska, Anna,Piasecki, Egbert,Pietka-Ottlik, Magdalena
, (2017/06/28)
A reaction of bis[(2-chlorocarbonyl)phenyl] diselenide with various mono and bisnucleophiles such as aminophenols, phenols, and amines have been studied as a convenient general route to a series of new antimicrobial and antiviral diphenyl diselenides. The compounds, particularly bis[2-(hydroxyphenylcarbamoyl)]phenyl diselenides and reference benzisoselenazol-3(2H)-ones, exhibited high antimicrobial activity against Gram-positive bacterial species (Enterococcus spp., Staphylococcus spp.), and some compounds were also active against Gram-negative E. coli and fungi (Candida spp., A. Niger). The majority of compounds demonstrated high activity against human herpes virus type 1 (HHV-1) and moderate activity against encephalomyocarditis virus (EMCV), while they were generally inactive against vesicular stomatitis virus (VSV).
Synthesis of new alkylated and methoxylated analogues of ebselen with antiviral and antimicrobial properties
Pietka-Ottlik, Magdalena,Burda-Grabowska, Ma?gorzata,Wo?na, Marta,Waleńska, Joanna,Kaleta, Rafa?,Zaczyńska, Ewa,Piasecki, Egbert,Giurg, Miros?aw
, p. 546 - 556 (2017/03/14)
A series of new mono and disubstituted alkylated and methoxylated benzisoselanzol-3(2H)-ones and bis(2-carbamoylaryl)diselenides were prepared in yields ranging from 55% to 95% starting from anthranilic acid and were evaluated for antiviral and antimicrobial activity. The compounds exhibited antiviral activity against Human herpes virus 1 and Encephalomyocarditis virus as well as antimicrobial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Candida albicans. (Chemical Equation Presented).
Identification of methionine aminopeptidase 2 as a molecular target of the organoselenium drug ebselen and its derivatives/analogues: Synthesis, inhibitory activity and molecular modeling study
W?glarz-Tomczak, Ewelina,Burda-Grabowska, Ma?gorzata,Giurg, Miros?aw,Mucha, Artur
supporting information, p. 5254 - 5259 (2016/11/09)
A collection of twenty-six organoselenium compounds, ebselen and its structural analogues, provided a novel approach for inhibiting the activity of human methionine aminopeptidase 2 (MetAP2). This metalloprotease, being responsible for the removal of the amino-terminal methionine from newly synthesized proteins, plays a key role in angiogenesis, which is essential for the progression of diseases, including solid tumor cancers. In this work, we discovered that ebselen, a synthetic organoselenium drug molecule with anti-inflammatory, anti-oxidant and cytoprotective activity, inhibits one of the main enzymes in the tumor progression pathway. Using three-step synthesis, we obtained twenty-five ebselen derivatives/analogues, ten of which are new, and tested their inhibitory activity toward three neutral aminopeptidases (MetAP2, alanine and leucine aminopeptidases). All of the tested compounds proved to be selective, slow-binding inhibitors of MetAP2. Similarly to ebselen, most of its analogues exhibited a moderate potency (IC50= 1–12 μM). Moreover, we identified three strong inhibitors that bind favorably to the enzyme with the half maximal inhibitory concentration in the submicromolar range.
Diselenobis-benzoic acid amides of primary and secondary amines and processes for the treatment of diseases in humans caused by a cell injury
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, (2008/06/13)
The present invention relates to new diselenobis-benzoic acid amides of primary and secondary amines of the general formula (I): STR1 and processes for the treatment of diseases in humans caused by a cell injury.
