一锅法点击化学：用于合成作为抗结核药物的2-巯基苯并咪唑连接香豆素基三唑的三组分反应。
One pot Click chemistry: A three component reaction for the synthesis of 2-mercaptobenzimidazole linked coumarinyl triazoles as anti-tubercular agents.
作者信息
Anand Ashish, Kulkarni Manohar V, Joshi Shrinivas D, Dixit Sheshagiri R
机构信息
Department of Studies in Chemistry, Karnatak University, Pavate Nagar, Dharwad 580003, Karnataka, India.
Department of Studies in Chemistry, Karnatak University, Pavate Nagar, Dharwad 580003, Karnataka, India.
出版信息
Bioorg Med Chem Lett. 2016 Oct 1;26(19):4709-4713. doi: 10.1016/j.bmcl.2016.08.045. Epub 2016 Aug 20.
2-Propargylthiobenzimidazole 1, 4-bromomethyl coumarins/1-aza-coumarins 2/3 and sodium azide have been reacted in one pot under Click chemistry conditions to give exclusively 1,4-disubstituted triazoles 5a-n. Anti-tubercular assays against M. tuberculosis (H37Rv) coupled with in silico molecular docking studies indicated that dimethyl substituents 5c and 5d showed promising activity with higher C-score values.
2-丙炔基硫代苯并咪唑、1,4-溴甲基香豆素/1-氮杂香豆素2/3与叠氮化钠在点击化学条件下一锅反应，专一性地生成1,4-二取代三唑5a-n。针对结核分枝杆菌（H37Rv）的抗结核活性测定以及计算机辅助分子对接研究表明，二甲基取代物5c和5d表现出有前景的活性，且具有更高的C分数值。
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