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[1,2,4]Triazolo[4,3- a ]quinoxaline: synthesis, antiviral, and antimicrobial activities
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2011-08-06 , DOI: 10.1007/s00044-011-9753-7
Morkos A. Henen , Serry A. A. El Bialy , Fatma E. Goda , Magda N. A. Nasr , Hassan M. Eisa

A series of novel [1,2,4]triazolo[4,3-a]quinoxaline derivatives and their isosteres, pyrimido-quinoxaline, were synthesized as potential antiviral and antimicrobial agents. The new compounds were synthesized via aromatic nucleophilic substitution of 4-chloro-8-methyl[1,2,4]triazolo[4,3-a]quinoxaline-1-amine with different amines and triazole-2-thiol. Some of the synthesized compounds were subjected to antiviral and cytotoxicity screening using plaque-reduction assay. Most of the tested compounds exhibited cytotoxicity at concentration 160 μg/ml and compound 8b showed promising antiviral activity. In vitro antimicrobial screening against different pathogenic organisms using agar diffusion method demonstrated that compounds 4d, 6c, 7b, and 8a exhibit antibacterial and/or antifungal activities.

中文翻译:

[1,2,4]三唑并[4,3- a]喹喔啉:合成,抗病毒和抗菌活性

合成了一系列新颖的[1,2,4]三唑并[4,3- a ]喹喔啉衍生物及其同等异构体,嘧啶-喹喔啉,作为潜在的抗病毒药和抗菌剂。通过芳族亲核取代4-氯-8-甲基[1,2,4]三唑并[4,3 - a ]喹喔啉-1-胺与不同的胺和三唑-2-硫醇合成新化合物。使用噬斑减少测定法对一些合成的化合物进行了抗病毒和细胞毒性筛选。大多数测试化合物在浓度为160μg/ ml时显示出细胞毒性,化合物8b显示出有希望的抗病毒活性。使用琼脂扩散法对不同病原微生物进行体外抗菌筛选表明,化合物4d图6c7b8a显示出抗菌和/或抗真菌活性。
更新日期:2011-08-06
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