6512-83-0Relevant articles and documents
Synthesis and biological evaluation of new nitrogen-containing diselenides
Nascimento, Vanessa,Ferreira, Natasha L.,Canto, R?mulo F.S.,Schott, Karen L.,Waczuk, Emily P.,Sancineto, Luca,Santi, Claudio,Rocha, Jo?o B.T.,Braga, Antonio L.
, p. 131 - 139 (2014)
The antioxidant properties of organoselenium compounds have been extensively investigated with the aim of developing new drugs, since oxidative stress is responsible for a variety of chronic human diseases. Herein, we reported the synthesis of new nitrogen-containing diselenides by a simple and efficient synthetic route. The products were obtained in good to excellent yields and their identification and characterization were achieved by NMR and HRMS techniques. The new derivatives may represent promising structures with different biological activities, which can act against oxidative stress through diverse mechanisms of action. The glutathione peroxidase-like assay (GPx-like activity) of the new synthesized compounds indicated that they reduced H2O2to water at the expense of PhSH. The best results were obtained with diselenide 2b, which was 9 times more active than the standard organoselenium drug ebselen and, in contrast, this compound was not reduced by hepatic TrxR. All of the new compounds inhibited Fe(II)-induced TBARS.
Structure-Guided Discovery of the Novel Covalent Allosteric Site and Covalent Inhibitors of Fructose-1,6-Bisphosphate Aldolase to Overcome the Azole Resistance of Candidiasis
Cao, Hongxuan,Chen, Han,Han, Xinya,Huang, Yunyuan,Liu, Jiaqi,Peng, Chao,Rao, Li,Ren, Yanliang,Sheng, Chunquan,Su, Chen,Tu, Jie,Wan, Chen,Wan, Jian,Wen, Wuqiang
, p. 2656 - 2674 (2022/02/09)
Fructose-1,6-bisphosphate aldolase (FBA) represents an attractive new antifungal target. Here, we employed a structure-based optimization strategy to discover a novel covalent binding site (C292 site) and the first-in-class covalent allosteric inhibitors
Benzoselenazolone compound and application thereof and bactericide
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, (2021/01/24)
The invention relates to the field of antifungal drugs, and discloses a benzoselenazolone compound and application thereof and a bactericide, and the benzoselenazolone compound has a structural general formula shown in a formula (I). The benzoselenazolone compound provided by the invention can take candida albicans fructose-1, 6-diphosphate aldolase (Ca-FBA-II) as a target spot to inhibit the activity of the candida albicans fructose 1, 6-diphosphate aldolase (Ca-FBA-II), and has a good resistance effect on drug-resistant bacteria generated by taking cytochrome P450 as an action target.
SELENIUM-CONTAINING ISOXAZOLAMINE COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF
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Paragraph 0067-0070, (2021/09/26)
The present invention disclosed a series of novel selenium-containing isoxazolamine derivatives as shown in formula I, which could regulate the generation and/or activity of TNF-α and ferroptosis-like cell death. The present invention also disclosed the preparation method and the use thereof in preparing a drug for treating the diseases mediated by TNF-α and/or iron-dependent cell death.
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.
High-throughput tandem-microwell assay for ammonia repositions FDA-Approved drugs to inhibit Helicobacter pylori urease
Fang, Houqin,Huang, Shengshuo,Li, Fangzheng,Liao, Lujian,Liu, Fan,Liu, Qi,Wu, Fang,Wu, Xin-Yan,Xiao, Zhuping,Xu, Jinyi,Yu, Jing,Zhang, Yan-Xia,Zhou, Yueyang
, (2021/11/01)
To date, little attempt has been made to develop new treatments for Helicobacter pylori (H. pylori), although the community is aware of the shortage of treatments for H. pylori. In this study, we developed a 192-tandem-microwell-based high-throughput assay for ammonia that is a known virulence factor of H. pylori and a product of urease. We could identify few drugs, that is, panobinostat, dacinostat, ebselen, captan, and disulfiram, to potently inhibit the activity of ureases from bacterial or plant species. These inhibitors suppress the activity of urease via substrate-competitive or covalent-allosteric mechanism, but all except captan prevent the antibiotic-resistant H. pylori strain from killing human gastric cells, with a more pronounced effect than acetohydroxamic acid, a well-known urease inhibitor and clinically used drug for the treatment of bacterial infection. This study offers several bases for the development of new treatments for urease-containing pathogens and to study the mechanism responsible for the regulation of urease activity.
Pyrimidine-selenium benzoic acid derivative as well as preparation method and application thereof as herbicide
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Paragraph 0045-0046, (2021/11/19)
The invention belongs to the technical field of herbicides, and particularly relates to a pyrimidine-selenium benzoic acid derivative as well as a preparation method and application thereof as a herbicide. The compound is subjected to nucleophilic substit
Crystal form of 1, 4-[bis(1, 2-benzisoselenazole-3(2H)-ketone)] butane and preparation method and application thereof
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Paragraph 0052-0059, (2021/01/04)
The crystal form I of 1, 4-[bis(1, 2-benzisoselenazole-3(2H)-ketone)] butane is radiated by Cu-Kalpha, and X-ray powder diffraction expressed by a 2theta angle has characteristic peaks at 6.17+/-0.20degree, 12.28+/-0.20 degree, 18.44+/-0.20 degree, 25.92+/-0.20 degree and 30.95+/-0.20 degree. The crystal form has good stability, is not suitable for crystal transformation, is beneficial to preparation, use, transportation and storage of pharmaceutical compositions and preparations, and fully guarantees the medication safety and the drug quality. In addition, the crystal form has high solubility, reasonable bioavailability, low toxicity and excellent tumor inhibition activity.
Ultrasound-assisted synthesis of alkali metals diselenides (M2Se2) and their application for the gram-scale preparation of 2,2’-diselenobis(benzoic acid)
Krasowska, Dorota,Begini, Francesca,Santi, Claudio,Mangiavacchi, Francesca,Drabowicz, Jozef,Sancineto, Luca
, p. 24 - 37 (2020/02/13)
A simple and efficient method to convert elemental selenium into alkali metal diselenide was developed. The use of selenium and metal borohydride in a molar ratio of 1 to 0.125 in the presence of base, under “on water” conditions and ultrasound activation permitted the reduction of Se into Se22- to be completed within minutes. Thus obtained metal diselenide aqueous solution was then used in the multigram scale synthesis of 2,2’-diselenobis(benzoic acid) (DSBA) a valuable building block for the development of diverse and pivotal selenorganic compounds.
1,2-BENZISOSELENAZOL-3(2H)-ONE AND 1,2-BENZISOTHIAZOL-3(2H)-ONE DERIVATIVES AS BETA-LACTAM ANTIBIOTIC ADJUVANTS
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Paragraph 0186; 0187, (2019/10/04)
Provided herein are compositions and methods useful in the treatment of beta-lactam antibiotic resistant bacteria.
