Trifluoromethylpyridine 1,3,4-Oxadiazole Derivatives: Emerging Scaffolds as Bacterial Agents

Gang Yu; Shunhong Chen; Shengxin Guo; Bixue Xu; Jian Wu

doi:10.1021/acsomega.1c04472

Trifluoromethylpyridine 1,3,4-Oxadiazole Derivatives: Emerging Scaffolds as Bacterial Agents

ACS Omega. 2021 Nov 9;6(46):31093-31098. doi: 10.1021/acsomega.1c04472. eCollection 2021 Nov 23.

Authors

Gang Yu^{1

2

3}, Shunhong Chen¹, Shengxin Guo¹, Bixue Xu^{2

3}, Jian Wu¹

Affiliations

¹ State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, China.
² State Key Laboratory for Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550014, China.
³ The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences/Guizhou Provincial Engineering Research Center for Natural Drugs, Guiyang 550014, China.

Abstract

A new class of trifluoromethylpyridine 1,3,4-oxadiazole derivatives (6a-6v) was obtained, and their antibacterial activities were evaluated. Some of them exhibited good activity, particularly 6a, which had the highest in vitro activity against Ralstonia solanacearum (R. solanacearum) and Xanthomonas axonopodis pv. citri (Xac). The half-maximal effective concentrations (EC₅₀) were 26.2 and 10.11 μg/mL, respectively, which were lower than those of commercial thiodiazole copper (97.2 and 35.3 μg/mL, respectively). Furthermore, 6q showed much higher activity against Xanthomonas oryzae pv. oryzae (Xoo) with an EC₅₀ value of 7.2 μg/mL; this was superior to bismerthiazol (57.2 μg/mL). Collectively, our findings provide a foundation for the development of trifluoromethylpyridine 1,3,4-oxadiazole derivatives.