To improve the physical and chemical properties of phenazine-1-carboxylic acid (PCA) and find higher antifungal compounds, a series of PCA amide analogues were designed and synthesized and their structures were confirmed by 1H NMR, HRMS, and X-ray. Most compounds showed some antifungal activities in vitro. Particularly, compound 3d exhibited inhibition effect against Pyriculariaoryzac Cavgra with EC50 value of 28.7 μM and compound 3q exhibited effect against Rhizoctonia solani with EC50 value of 24.5 μM, more potently active than that of the positive control PCA with its EC50 values of 37.3 μM (Pyriculariaoryzac Cavgra) and 33.2 μM (Rhizoctonia solani), respectively.
Keywords: Phenazine-1-carboxylic acid (PCA); amide; analogue; antifungal activity; synthesis.