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新型 5,6-二氢-吲哚并[1,2-a]喹喔啉衍生物的合成与抗真菌活性。

Synthesis and antifungal activities of novel 5,6-dihydro-indolo[1,2-a]quinoxaline derivatives.

机构信息

Laboratory of Pharmaceutical Design and Synthesis, College of Sciences, Xinong Road 22#, Northwest A&F University, Yangling 712100, China.

出版信息

Eur J Med Chem. 2011 May;46(5):1919-25. doi: 10.1016/j.ejmech.2011.02.035. Epub 2011 Feb 23.

Abstract

A series of new 5,6-dihydro-indolo[1,2-a]quinoxaline derivatives has been prepared in moderate to excellent yields from 2-(indol-1-yl)phenylamines with aromatic aldehydes by an efficient and economical iron-catalyzed Pictet-Spengler reaction. Meanwhile, as compared with hymexazol, a commercially available agricultural fungicide at the concentration of 50 μg/mL, some 5,6-dihydro-indolo[1,2-a]quinoxalines exhibited promising antifungal activities in vitro against the phytopathogenic fungi, and might be considered as novel promising lead candidates for further design and synthesis of agricultural fungicides.

摘要

一系列新的 5,6-二氢吲哚并[1,2-a]喹喔啉衍生物已通过高效经济的铁催化Pictet-Spengler 反应从 2-(吲哚-1-基)苯胺与芳香醛以中等至优异的产率制备。同时,与 50μg/mL 的市售农业杀菌剂 hymexazol 相比,一些 5,6-二氢吲哚并[1,2-a]喹喔啉在体外对植物病原真菌表现出有希望的抗真菌活性,并且可能被认为是进一步设计和合成农用杀菌剂的新型有前途的先导候选物。

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