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Anti-tubercular activity of novel class of spiropyrrolidine tethered indenoquinoxaline heterocyclic hybrids.
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2020-03-26 , DOI: 10.1016/j.bioorg.2020.103799
Natarajan Arumugam 1 , Abdulrahman I Almansour 1 , Raju Suresh Kumar 1 , Shatha Ibrahim Alaqeel 2 , Vagolu Siva Krishna 3 , Dharmarajan Sriram 3
Affiliation  

A series of structurally intriguing novel class of spiropyrrolidine tethered quinoxaline heterocyclic hybrids has been achieved in excellent yields employing ionic liquid accelerated multicomponent 1,3-dipolar cycloaddition reaction strategy. β-Nitrostyrenes were used as dipolarophiles, while the 1,3-dipole component was the azomemthine ylide, generated in situ from indenoquinoxaline and l-phenylalanine. The reaction provided three new bonds and four contiguous stereocenter with full distereomeric control. In vitro activity of these spiroheterocyclic hybrids against Mycobacterium tuberculosis H37Rv using MABA assay revealed that the compound with nitro group on the phenyl ring is the most active candidate (1.56 µg/mL) among the other analogues of the series and has an activity similar to that of the standard drug, Ethambutol.

中文翻译:

新型螺吡咯烷拴系的茚并喹喔啉杂环杂种的抗结核活性。

使用离子液体加速多组分1,3-偶极环加成反应策略,已以优异的产率获得了一系列结构吸引人的新型螺吡咯烷系链的喹喔啉杂环杂化物。β-硝基苯乙烯被用作双极性亲和剂,而1,3-偶极成分是由茚并喹喔啉和1-苯丙氨酸原位生成的阿兹美辛碱。该反应提供了三个新的键和四个连续的立体中心,并具有完全的对映体控制。使用MABA分析,这些螺旋杂环杂种对结核分枝杆菌H37Rv的体外活性表明,苯环上带有硝基的化合物是该系列其他类似物中活性最高的候选化合物(1.56 µg / mL),其活性与之相似。标准药物乙胺丁醇。
更新日期:2020-04-20
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