Photostable 1-Trifluoromethyl Cinnamyl Alcohol Derivatives Designed as Potential Fungicides and Bactericides.

Abstract

In the current work, a series of 1-trifluoromethyl cinnamyl alcohol derivatives were designed and synthesized and their antifungal activities were evaluated. The bioassay result showed that most compounds exhibited excellent antifungal activity in vitro at 10 μg mL-1. Next, photostable and easily synthesized compound 2 with broad-spectrum antifungal activity in vitro was selected as a potential candidate to evaluate its antibacterial and antifungal activities. The EC50 values of compound 2 against eight fungal plant pathogens in vitro ranged from 3.806 to 17.981 μg mL-1; at the same time, compound 2 could effectively control Podosphaera xanthii, Odium heveae Steinm, Puccinia striiformis West, and Puccinia sorghi in pot experiments. In addition, compound 2 exhibited excellent antibacterial activities in vitro and in vivo against Xanthomonas oryzae pv. oryzae. Furthermore, the absorption and translocation of compound 2 in wheat plants were determined by the high-performance liquid chromatography method. The result showed that compound 2 could be translocated acropetally as well as basipetally in wheat plants. Finally, it was found that compound 2 had no cross-resistance with carbendazim, azoxystrobin, and boscalid.