Synthesis and bioactivities of phenazine-1-carboxylic piperazine derivatives.,Natural Product Research

当前位置： X-MOL 学术 › Nat. Prod. Res. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Synthesis and bioactivities of phenazine-1-carboxylic piperazine derivatives.
Natural Product Research ( IF 1.9 ) Pub Date : 2019-01-30 , DOI: 10.1080/14786419.2018.1556656
Fei Han ₁ , Ru Yan _{1,

2} , Min Zhang _{1,

2} , Zhu Xiang _{1,

2} , Qinglai Wu _{1,

2} , Junkai Li _{1,

2}

Affiliation

Phenazine-1-carboxylic acid (PCA) as a natural product which has significant inhibition effects against many soil-borne fungal phytopathogens in agricultural application and has been registered in China as the fungicide against rice sheath blight. In order to find new higher fungicidal activities lead compounds and develop new eco-friendly agrochemicals, we introduced substructure piperazines which also have high biological activity into PCA, designed and synthesized a series of phenazine-1-carboxylic piperazine derivatives, and their structures were confirmed by 1H NMR and HRMS. Most compounds exhibited certain in vitro fungicidal activities. In particular, Compounds 5r exhibited the activity against all the tested pathogenic fungi, such as Rhizoctonia solani, Alternaria solani, Fusarium oxysporum, Fusarium graminearum, Pyricularia oryzac Cavgra, with the EC50 value of 24.6μM, 42.9μM, 73.7μM, 73.8μM, 34.2μM, respectively, more potent activities than PCA (33.2μM, 81.5μM, 186.5μM, 176.4μM, 37.3μM). This result provided a highly active lead compound for the further structure optimization design.

更新日期：2019-01-30

点击分享查看原文

点击收藏

阅读更多本刊最新论文本刊介绍/投稿指南

全部期刊列表>>