• Applied Biological Chemistry
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• v.38 no.2
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• pp.163-167
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• 1995

New twenty 2-(n-octyl)-3-(n-propyl)isothiourea derivatives(S) were synthesized which is modified from the insecticidal Buprofezine (Applaud) in the selective insecticidal activities in-vitro against Diamond-Back moth (Plutella Xylostella Linnaeus). The structure activity relationships(SAR) between the insecticidal activity$(pI_{50})$ and a various physicochemical parameters of the substituent(Z) of S were analyzed by the multiple regression technique. The activities would depend largely on the MR, ${\pi}$ and $L_1$ parameters. The SAR was rationalized by parabolic function of MR, ${\pi}$ and $L_1$ constant, where the optimal values of the constants were $L_1=5.22{{\AA}}$, $MR=15.70\;Cm^3/mol$ and ${\pi}=1.60$, respectively. The steric effects play an important role in determining insecticidal activity. The SAR suggest that the S derivatives having a substituents with a small breadth and an appropriate length as Z group showed potent activity. From the results, the iso-propyl group(Z) substituent (5) with three carbon atom was the most effective compound.