Pest Management Science (2012) 68, 10-15

Jin-Hao Zhao, Zong-Cheng Wang, Ming-Hua Ji, Jing-Li Cheng, Guo-Nian Zhu and Chuan-Ming Yu (2012)
Synthesis and bioactivity evaluation of novel spiromesifen derivatives
Pest Management Science 68 (1), 10-15
Abstract: BACKGROUND: The development of environmentally friendly and novel structural pesticides is now an area of intense research in the agriculture field. Spirocyclic tetronic acids such as spiromesifen are typical compounds of this kind. In order to discover novel compounds with improved and broader-spectrum insecticidal activities, a series of spiromesifen derivatives were synthesised and bioassayed.
RESULTS: The derivatives were identified by ¹H NMR and MS. Preliminary bioassays demonstrated that some bioactivities of compounds 5a to 5u were better and had a broader spectrum than the lead compound spiromesifen. Moreover, these compounds showed better insecticidal activities against Mythimna separata and Aphis fabae than acaricidal activities against Tetranychus cinnabarinus. Furthermore, LC₅₀ of 5s against Aphis fabae reached 1.09 mg L⁻¹. At the same time, compounds 5g, 5i, 5k and 5r also warrant further study because of their superior bioactivities to spiromesifen. What is more, suitable carbon chain length in the 4-position ester and the log P value of these spiromesifen derivatives dramatically influenced their insecticidal activities. Butyric or pentanoic ester and a log P value of 4.0-6.0 may be preferred.
CONCLUSION: The present work demonstrates that some spiromesifen derivatives can be used as potential lead compounds for developing novel insecticides and acaricides.
(The abstract is excluded from the Creative Commons licence and has been copied with permission by the publisher.)
Link to article at publishers website

Research topic(s) for pests/diseases/weeds:
control - general

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Pest and/or beneficial records:

Beneficial	Pest/Disease/Weed	Crop/Product	Country	Quarant.
	Aphis fabae
	Tetranychus cinnabarinus
	Mythimna separata