Azaanalogues of ebselen as antimicrobial and antiviral agents: synthesis and properties

Synthesis of new alkylated and methoxylated analogues of ebselen with antiviral and antimicrobial properties

“…A similar tendency was observed in our previous studies. [24][25][26] Generally, benzisoselenazol-3(2H)-ones 4 were more active than corresponding diselenides 6. The results of screening of benzisoselenazol-3(2H)-ones 4 toward HHV-1 are particularly interesting.…”

“…[8][9][10][11][12][13][14][15]20,21 Ebselen (2-phenylbenzisoselenazol-3(2H)-one) and its analogues have received particular attention as glutathione peroxidase mimics, 8,11,15 antioxidant and anti-inflammatory agents. [13][14][15] Furthermore, the continuing interest in this class of compounds has led to the development of various structures with antiviral [22][23][24][25][26] and antimicrobial [24][25][26][27] properties. In this work we report a convenient synthetic route to a series of new alkylated and methoxylated benzisoselanazol-3(2H)-ones 4 and bis(2-carbamoylaryl)diselenides 6 which were tested for antiviral and antimicrobial activity in biological studies.…”

New Organoselenium Compounds Active against Pathogenic Bacteria, Fungi and Viruses

“…7,8) Moreover, some of these compounds, particularly their 7-azaanalogues, exhibited high inhibitory activity against pathogenic bacteria, fungi and viruses. 9) In this paper we report synthesis, chemical properties as well as inhibitory activity against viruses, bacteria and fungi of ebselen analogues (2-6), having in 2-position alkyl groups (2) or containing oxaalkyl or azaalkyl functions (3)(4)(5)(6). We wanted to answer the question whether the introduction of additional polar functions to alkyl substituent in 2-position can have the influence on biological activity of tested compounds.…”

Synthesis and Biological Activities of Novel 2,5-Disubstituted- 1,3,4-thiadiazole Derivatives

“…这一结论对于通过结 构变化寻找更好性能的硒类化合物的药物具有重要的 指导意义. 由于依布硒的溶解性较差 [11] , 细胞内的吸收 较低 [12] , 所以为了提高其溶解度和活性、细胞内的吸收 和疗效, 近年来许多苯并异硒唑酮衍生物被相继合成出 来, 并且研究表明, 它们具有抗癌 [7] 、抗氧化 [13] 、抗菌、 抗病毒 [9,14] 、抑制阿尔茨海默氏病 [15,16] 等活性. Figure 1 Structure of ebselen 改进溶解性的常规方法是引入额外的杂原子, 或增 加旋转键的数目 [17] .…”