Synthesis and Fungicidal Activity of β-Carboline Alkaloids and Their Derivatives

摘要

A series of β-Carboline derivatives were designed, synthesized, and evaluated for their fungicidal activities in this study. Several derivatives electively exhibited fungicidal activities against some fungi. Especially, compound >F5 exhibited higher fungicidal activity against Rhizoctonia solani(53.35%) than commercial antiviral agent validamycin (36.4%); compound >F16 exhibited high fungicidal activity against Oospora citriaurantii ex Persoon(43.28%). Some of the alkaloids and their derivatives (compounds >F4 and >F25) exhibited broad-spectrum fungicidal activity. Specifically, compound >F4 exhibited excellent high broad-spectrum fungicidal activity in vitro, and the curative and protection activities against P. litchi in vivo reached 92.59% and 59.26%, respectively. The new derivative, >F4, with optimized physicochemical properties, obviously exhibited higher activities both in vitro and in vivo; therefore, >F4 may be used as a new lead structure for the development of fungicidal drugs.