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Synthesis and biological evaluation of 2-(4-substituted benzene-1-sulfonyl)-N'-(substituted-1-sulfonyl)acetohydrazide as antibacterial agents

Pei Li, Junliang Zhou, Yan Liu, and Xiang Wang

Qiandongnan Engineering and Technology Research Center for Comprehensive Utilization of National Medicine, Kaili University, Kaili, People’s Republic of China

 

E-mail: pl19890627@126.com

Received: 20 January 2020  Accepted: 27 June 2020

Abstract:

In this study, a series of new sulfone derivatives containing a sulfonohydrazide moiety were synthesized and their structures were determined using 1H NMR, 13C NMR, and HRMS. Then, the in vitro antibacterial activities against Xanthomonas oryzae pv. oryzae (Xoo) and Xanthomonas axonopodis pv. citri (Xac) were evaluated by performing turbidimeter test. Bioactivity results showed that compound 2-(4-fluorobenzene-1-sulfonyl)-N′-(4-fluorobenzene-1-sulfonyl)acetohydrazide (5g) revealed the best antibacterial activities against Xoo and Xac, with the 50% effective concentration (EC50) values of 25 and 36 µg/mL, respectively, which were superior to those of thiodiazole copper (110 and 230 µg/mL, respectively) and bismerthiazol (84 and 146 µg/mL, respectively).

Keywords: Sulfone; Sulfonohydrazide; Synthesis; Antibacterial activity

Full paper is available at www.springerlink.com.

DOI: 10.1007/s11696-020-01271-6

 

Chemical Papers 74 (12) 4559–4565 (2020)

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