| Project/Area Number |
60470136
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| Research Category |
Grant-in-Aid for General Scientific Research (B)
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| Allocation Type | Single-year Grants |
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| Research Field |
製造化学・食品
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| Research Institution | Kyoto University |
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Principal Investigator |
FUJITA Toshio Faculty of Agriculture, Kyoto University, Professor, 農学部, 教授 (90026427)
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| Co-Investigator(Kenkyū-buntansha) |
NAKAGAWA Yoshiaki Faculty of Agriculture, Kyoto University, Instructor, 濃学部, 助手 (80155689)
NISHIMURA Keiichiro Faculty of Agriculture, Kyoto University, Instructor, 濃学部, 助手 (70026558)
IWAMURA Hajime Faculty of Agriculture, Kyoto University, Associate Professor, 濃学部, 助教授 (30026570)
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| Project Period (FY) |
1985 – 1986
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| Project Status |
Completed (Fiscal Year 1986)
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| Budget Amount *help |
¥5,400,000 (Direct Cost: ¥5,400,000)
Fiscal Year 1986: ¥700,000 (Direct Cost: ¥700,000)
Fiscal Year 1985: ¥4,700,000 (Direct Cost: ¥4,700,000)
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| Keywords | Insect juvenile hormone / Quantitative structure-activity relationship / Pyrethroids / Benzoylphenylureas / ベンゾイルフェニルウレア |
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| Research Abstract |
(1) Based on the quantitative structure-activity relationship analysis of the terpenoid insect juvenile hormone (JH) mimics, a non-terpenoid class of JH-active compounds, 4-phenoxyphenoxy- and 4-benzylphenoxyacetaldoxime O-ether was developed. Further by alteration of the aldoxime moiety of the molecule, we found 4-phenoxyphenoxypropionaldoxime O-ether type of compounds to be highly active. Quantitative structure-activity analyses of the series of the compounds showed that the molecular dimensions or shape of the molecules are important factors for high JH activity, together with a position specific electronic or hydrophobic property.
(2) A set of pyrethroid analogs where the alcohol and acidic moiety were modified was prepared. Insecticidal activity against the American cockroach and neurophysiological activity in excised nerve preparations were determined for each compound. Variations in these activities were shown to be mostly determined by steric dimensions and hydrophobicity of the molecular components. Their insecticidal activity was nicely correlated with the nerve activity. Voltage clamp studies revealed that the compounds greatly increase the sodium current. Thus, their insecticidal effect was concluded to de due to lesion in the nerve conduction system in insects, which was brought about by modulation of the sodium channels.
(3) A series of insecticidal benzoylaminothiadiazoles was prepared to examine their structure- activity relationships. The activity against mosquito (Culex pipiens) and rice stem borer (Chilo suppressalis) larvae was found to be risen by introducing an electron-withdrawing substituent into the para position of the terminal benzene. Furthermore, a comparison of the structure-activity profile with that of the structurally analogus insecticides, benzoyl-phenylureas, revealed that the hydrophobic and/or steric effects on activity are different between the two series of compounds.
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