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- Title
Synthesis and bioactivities of phenazine-1-carboxylic piperazine derivatives.
- Authors
Han, Fei; Yan, Ru; Zhang, Min; Xiang, Zhu; Wu, Qinglai; Li, Junkai
- Abstract
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.
- Subjects
CHINA; PIPERAZINE; RICE sheath blight; RHIZOCTONIA solani; PATHOGENIC fungi; FUSARIUM oxysporum; ALTERNARIA
- Publication
Natural Product Research, 2020, Vol 34, Issue 9, p1282
- ISSN
1478-6419
- Publication type
Academic Journal
- DOI
10.1080/14786419.2018.1556656