Mori Kotaro, Miyashita Masahiro, Mori Soichirou, Shibata Norio, Ikeguchi Mitsunori, Nakagawa Yoshiaki
Division of Applied Life Sciences, Graduate School of Agriculture, Kyoto University.
Department of Nanopharmaceutical Sciences, Graduate School of Engineering, Nagoya Institute of Technology.
J Pestic Sci. 2025 Aug 20;50(3):81-86. doi: 10.1584/jpestics.D25-040.
-(3-Phenylisoxazol-5-yl)benzamides (5-benzoylamino-3-phenylisoxazoles: IOXs) with various substituents at two benzene rings were synthesized, and the chitin synthesis inhibition was measured in the cultured integumentary system of . Larvicidal effects against and were also examined, and the larvicidal activity in terms of the 50% lethal dose (LD) was determined for some compounds. Among IOXs with various substituents at the benzoyl moiety, 2,6-difluoro-substituted (2,6-F) benzoyl analogs showed the highest chitin synthesis activity. The larvicidal activities against and were 1/138 and 1/35 that of diflubenzuron, a representative benzoylphenylurea-type insecticide, respectively. In a further study, 2,6-F benzoyl analogs with various substituents at the phenyl moiety, such as Br, CF, CN, OEt, Ph, and alkyls (CH, Et, -Pr, -Bu, and -Bu), were synthesized, and their chitin synthesis inhibition in the integument and their larvicidal activity against were quantitatively measured. The introduction of bulky CF and -Bu at the phenyl moiety of 2,6-F benzoyl analog favorably enhanced the larvicidal activity against
合成了在两个苯环上带有各种取代基的-(3-苯基异恶唑-5-基)苯甲酰胺（5-苯甲酰氨基-3-苯基异恶唑：IOXs），并在……的培养体壁系统中测定了几丁质合成抑制作用。还检测了对……和……的杀幼虫效果，并确定了一些化合物的半数致死剂量（LD）的杀幼虫活性。在苯甲酰基部分带有各种取代基的IOXs中，2,6-二氟取代（2,6-F）的苯甲酰类似物表现出最高的几丁质合成活性。对……和……的杀幼虫活性分别是代表性的苯甲酰苯基脲类杀虫剂敌百虫的1/138和1/35。在进一步的研究中，合成了在苯基部分带有各种取代基（如Br、CF、CN、OEt、Ph和烷基（CH、Et、-Pr、-Bu和-Bu））的2,6-F苯甲酰类似物，并定量测定了它们在……体壁中的几丁质合成抑制作用及其对……的杀幼虫活性。在2,6-F苯甲酰类似物的苯基部分引入庞大的CF和-Bu有利于提高对……的杀幼虫活性
