To improve the insecticidal activities of fraxinellone, two series of fraxinellone-based N-(1,3-thiazol-2-yl)carboxamides containing 25 compounds were prepared by structural modification. Their structures were determined by melting point, optical rotation, IR, ¹H NMR and ESI-MS. The steric configurations of compounds 6i, 7d and 7i were unambiguously confirmed by X-ray diffraction further. The bioassay showed that compounds 6b and 6i exhibited more potent larvicidal and growth inhibitory activities against Plutella xylostella Linnaeus and Mythimna separata Walker, respectively. Moreover, compounds 6b and 6i also displayed low cytotoxicity to noncancerous mammalian cells. The structure–activity relationships (SARs) of all target compounds were also observed.

为了提高草胺酮的杀虫活性，通过结构修饰制备了两种含有25种化合物的草胺酮基N-（1,3-噻唑-2-基）羧酰胺系列。它们的结构由熔点，旋光度，IR，¹ H NMR和ESI-MS确定。通过X射线衍射进一步明确地确认了化合物6i，7d和7i的空间构型。生物测定表明，化合物6b和6i分别对小菜蛾（Plutella xylostella Linnaeus）和Mythimna separata Walker表现出更强的杀幼虫和生长抑制活性。此外，化合物6b和6i对非癌性哺乳动物细胞也显示出低细胞毒性。还观察到所有目标化合物的构效关系（SAR）。