Discovery of γ-lactam derivatives containing 1,3-benzodioxole unit as potential anti-phytopathogenic fungus agents

Abstract

A series of γ-lactam analogs containing 1,3-benzodioxole moiety were designed, and these derivatives were synthesized from the lead compound of lactam via a structural diversity-oriented synthesis, their structures were confirmed by ¹HNMR,¹³CNMR, ESI-MS spectrum. Their antifungal activities were evaluated against four serious and typically crop-threatening agricultural fungi, including Rhizoctonia solani, Alternaria tenuis Nees, Gloeosporium theae-sinensis, and Fusarium graminearum. Some of these derivatives exhibited activity against Alternaria tenuis Nees higher than that of commercial fungicides carbendazim, such as compounds 7a, 7b, and 7i, compared with the blank control, some of these derivatives showed good antifungal activities against Gloeosporium theae-sinensis and Fusarium graminearum. The systematic study provides evidences for further structural modification and application of lactam analogues as antifungal agents for agriculture.

Keywords: 1,3-Benzodioxole; Agricultural fungi; Antifungal activities; Diversity-oriented; γ-Lactam.