Design, synthesis and antifungal activities of novel pyrrole- and pyrazole-substituted coumarin derivatives

Abstract

We synthesized a series of novel pyrrole- and pyrazole-substituted coumarin derivatives and evaluated their antifungal activity against six phytopathogenic fungi in vitro. The primary assay results demonstrated that some designed compounds displayed potent activities. Among them, compounds 5g, 6a, 6b, 6c, 6d and 6h exhibited more effective control than Osthole against Cucumber anthrax and Alternaria leaf spot. Furthermore, compound 5g displayed stronger antifungal activity against Rhizoctorzia solani (EC₅₀ = 15.4 µg/mL) than positive control Osthole (EC₅₀ = 67.2 µg/mL).

Keywords: Aminocoumarin derivatives; Antifungal activity; Nitrogen-containing; Synthesis.