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Issue 12, 2018
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Design, synthesis, insecticidal activity and 3D-QSR study for novel trifluoromethyl pyridine derivatives containing an 1,3,4-oxadiazole moiety

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Abstract

A series of trifluoromethyl pyridine derivatives containing 1,3,4-oxadiazole moiety was designed, synthesized and bio-assayed for their insecticidal activity. The result of bio-assays indicated the synthesized compounds exhibited good insecticidal activity against Mythimna separata and Plutella xylostella, most of the title compounds show 100% insecticidal activity at 500 mg L−1 and >80% activity at 250 mg L−1 against the two pests. Compounds E18 and E27 showed LC50 values of 38.5 and 30.8 mg L−1 against Mythimna separata, respectively, which were close to that of avermectin (29.6 mg L−1); compounds E5, E6, E9, E10, E15, E25, E26, and E27 showed 100% activity at 250 mg L−1, which were better than chlorpyrifos (87%). CoMFA and CoMSIA models with good predictability were proposed, which revealed the electron-withdrawing groups with an appropriate bulk at 2- and 4-positions of benzene ring could enhance insecticidal activity.

Graphical abstract: Design, synthesis, insecticidal activity and 3D-QSR study for novel trifluoromethyl pyridine derivatives containing an 1,3,4-oxadiazole moiety

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Article information


Submitted
06 Jan 2018
Accepted
22 Jan 2018
First published
07 Feb 2018

This article is Open Access

RSC Adv., 2018,8, 6306-6314
Article type
Paper

Design, synthesis, insecticidal activity and 3D-QSR study for novel trifluoromethyl pyridine derivatives containing an 1,3,4-oxadiazole moiety

F. Z. Xu, Y. Y. Wang, D. X. Luo, G. Yu, S. X. Guo, H. Fu, Y. H. Zhao and J. Wu, RSC Adv., 2018, 8, 6306
DOI: 10.1039/C8RA00161H

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