Issue 59, 2020

Synthesis and biological activities of novel trifluoromethylpyridine amide derivatives containing sulfur moieties

Abstract

A series of trifluoromethylpyridine amide derivatives containing sulfur moieties (thioether, sulfone and sulfoxide) was designed and synthesized. Their antibacterial activities against Xanthomonas oryzae pv. oryzae (Xoo), Ralstonia solanacearum (R. solanacearum) and insecticidal activities against P. xylostella were evaluated. Notably, the half-maximal effective concentration (EC50) value of sulfone-containing compound F10 is 83 mg L−1 against Xoo, which is better than that of commercial thiodiazole copper (97 mg L−1) and bismerthiazol (112 mg L−1). Thioether-containing compounds E1, E3, E5, E6, E10, E11 and E13 showed much higher activities against R. solanacearum with the EC50 value from 40 to 78 mg L−1, which are much lower than that of thiodiazole copper (87 mg L−1) and bismerthiazol (124 mg L−1). Generally, most of the sulfone-containing compounds and sulfoxide-containing compounds showed higher activities against Xoo than that of the corresponding thioether-containing compound, but most of the thioether-containing compounds contributed higher antibacterial activities against R. solanacearum. Furthermore, title compounds E3, E11, E24 and G2 showed good insecticidal activities of 75%, 70%, 70% and 75%, respectively.

Graphical abstract: Synthesis and biological activities of novel trifluoromethylpyridine amide derivatives containing sulfur moieties

Supplementary files

Article information

Article type
Paper
Submitted
25 Aug. 2020
Accepted
17 Sept. 2020
First published
28 Sept. 2020
This article is Open Access
Creative Commons BY license

RSC Adv., 2020,10, 35658-35670

Synthesis and biological activities of novel trifluoromethylpyridine amide derivatives containing sulfur moieties

S. X. Guo, F. He, A. L. Dai, R. F. Zhang, S. H. Chen and J. Wu, RSC Adv., 2020, 10, 35658 DOI: 10.1039/D0RA07301F

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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