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具有甲基化咪唑烷环的手性吡虫啉衍生物对烟碱型乙酰胆碱受体的亲和力及杀虫活性

Affinity to the nicotinic acetylcholine receptor and insecticidal activity of chiral imidacloprid derivatives with a methylated imidazolidine ring.

作者信息

Nishiwaki Hisashi, Nagaoka Hikaru, Kuriyama Mituhiro, Yamauchi Satoshi, Shuto Yoshihiro

机构信息

Faculty of Agriculture, Ehime University, Ehime, Japan.

出版信息

Biosci Biotechnol Biochem. 2011;75(4):780-2. doi: 10.1271/bbb.100846. Epub 2011 Apr 22.

Abstract

Four imidacloprid derivatives with an asymmetrically methylated imidazolidine ring were synthesized. Their affinity to the nicotinic acetylcholine receptor of housefly Musca domestica and insecticidal activity against the housefly were measured. The compound with a 5R-methylated imidazolidine ring demonstrated intrinsic activity comparable to that of the unsubstituted compound. Most of the compounds were synergized by oxygenase inhibitors.

摘要

合成了四种具有不对称甲基化咪唑烷环的吡虫啉衍生物。测定了它们对家蝇烟碱型乙酰胆碱受体的亲和力以及对家蝇的杀虫活性。具有5R-甲基化咪唑烷环的化合物表现出与未取代化合物相当的内在活性。大多数化合物被氧化酶抑制剂增效。

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