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Paper | Regular issue | Vol 104, No. 10, 2022, pp.1809-1821
Published online, 19th August, 2022
DOI: 10.3987/COM-22-14725
Design, Synthesis, and Biological Activity Analysis of Novel Quinazolinyl Ether Derivatives Containing Piperidinamide Structure

Peijia Li, Yehui Yang, Nan Wu, Ya Yan, Lian An, Guangmin Tian, and Xiaoping Bao*

*State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Centre for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025, People’s Republic of China

Abstract

We designed and synthesized 27 ether derivatives containing quinazolinyl piperidinamide structures and characterized them by 1H NMR, 13C NMR, and HRMS. Bioassay results indicate that several target compounds display higher inhibition activities in vitro against phytopathogenic bacteria. For example, the EC50 of compound III-24 against Xanthomonas axonopodis pv. citri (Xac) is 33.9 µg/mL, which is double that of the commercialized bismerthiazol (EC50 = 75.5 µg/mL). Anti-Xac mechanisms show that compound III-24 exerts antibacterial effects by increasing the permeability of bacterial membranes, reducing their exopolysaccharide content, and inducing morphological changes in bacterial cells.