Synthesis and fungicidal activity of 1,3,4-oxadiazol-2-yl thioether derivatives containing a phenazine-1-carboxylic acid scaffold

Abstract

To find new higher fungicidal activities lead compounds and develop new eco-friendly agrochemicals, natural product phenazine-1-carboxylic acid (PCA) as scaffold, a series of 1,3,4-oxadiazol-2-yl thioether derivatives was synthesized and bio-assayed. The results reveal that most target compounds possessed moderate to good fungicidal activities against R. solani, S. sclerotioru and P. oryzac Cavgra. Compounds 6n and 6o exhibit more than 90% bioactivity against S. sclerotioru. The EC₅₀ value of compounds 6n and 6o are 11.16 and 30.47 μM respectively, in particular, compound 6n show equal activity against S. sclerotioru to PCA (10.49 μM). This result provides a valuable lead compound for further studies.

Keywords:

• Phenazine-1-carboxylic acid (PCA)
• 1,3,4-oxadiazol-2-yl thioether
• fungicidal activity
• derivatives
• synthesis

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This study was supported by Natural Science Foundation of China [No. 31672069] and Natural Science Foundation of Hubei Province [No. 2014CFA105].