• The Korean Journal of Pesticide Science
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• v.4 no.3
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• pp.27-33
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• 2000

N-Dimethoxyphosphinothionyl carbofuran, PSC, has a high insecticidal activity and low mammalian toxicity. Ten N-phosphinothionyl carbofuran derivatives were synthesized and their insecticidal activities were determined against brown plant hopper (Nilaparvata lugens), green peach aphid (Myzus persicae), diamondback moth (Plutella xylostella), and two-spotted spider mite (Tetranychus urticae). Green peach aphid, diamondback mea and brown plant hopper were controlled over 90% by application of 125 ppm, 125 ppm, and 63 ppm, respectively, of carbosulfan. Two hundred and fifty ppm of newly synthesized compounds could control most of brown plant hopper and diamondback moth. Especially, insecticidal activities of compound 10 against brown plant hopper, diamondback moth, and green peach aphid were similar to those of carbosulfan. Our results show that the newly synthesized derivatives of NV-phosphinothionyl carbofuran have a similar insecticidal activity to carbosulfan.

• The Korean Journal of Pesticide Science
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• v.2 no.2
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• pp.10-15
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• 1998

The bimolecular inhibition rate constants of carbofuran and N-dimethylphosphinothioyl carbofuran(PSC) to acetylcholinesterase(AChE) were $7.7{\times}10^{5}\;M^{-1}{\cdot}min^{-1}$ and $1.2{\times}10^{3}\;M^{-1}{\cdot}min^{-1}$, respectively. These results showed that PSC required a bioactivation process for its toxic action because it didn't inhibit the target enzyme effectively. The potency of PSC as an inhibitor of AChE increased when PSC and AChE were incubated with microsomes fortified with NADPH compared with microsome alone. Piperonyl butoxide(PBO) addition to these coupled systems greatly reduced the inhibition of the target enzyme by blocking the bioactivation process. In vivo inhibition study of mouse brain AChE, $I_{50}$ value for AChE was 28 mg/kg for PSC and the value increased to 57 mg/kg when PBO was pretreated. This result showed that cytochrome $P_{450}$ would also play a role in the bioactivation process of PSC in vivo. And conversioin of carbofuran from PSC was 55 % in a chemical oxidation system using meta-chloroperoxybenzoic acid. The oxidative activation of PSC to carbofuran was shown to be essential for showing its toxicological action and cytochrome $P_{450}$ was identified as an important enzyme which participated in this process.