Journal of Asian Natural Products Research ( IF 1.3 ) Pub Date : 2021-05-27 , DOI: 10.1080/10286020.2021.1925254 Wang-Yu Zhao 1, 2 , Chao-Fu Yang 2, 3 , Li-Juan Han 1, 2 , Bo Zhou 1, 2 , Ai-Juan Li 1, 2 , Lu-Lu Liu 1, 2 , Zi-Wei Zhang 1, 2 , Zi-Yu Wang 1, 2 , Wen-Jun Wu 2 , Ji-Wen Zhang 1, 2, 4
Abstract
In our previous studies, a kind of novel benzenesulfonamides was found to be a candidate insecticidal compounds. It was shown that propargyloxy and sulfonamide groups are pharmacodynamic groups. One hundred and twenty-six (126) naphthalenesulfonamides derivatives with propargyloxy functionality were designed and synthesized, and their insecticidal activities were determined. Some of them showed outstanding activity, with LC50 values as low as 0.202 mg ml−1, much lower than that of the positive control celangulin V (23.9 mg ml−1). In addition, the structure–activity relationships were discussed, and molecular docking was used to verify the binding mode of the compound and the target receptor.
中文翻译:
炔丙基氧基萘磺酰胺衍生物的设计、合成和杀虫活性
摘要
在我们之前的研究中,发现一种新型苯磺酰胺是一种候选的杀虫化合物。显示炔丙基氧基和磺酰胺基团是药效学基团。设计合成了一百二十六 (126) 种具有炔丙基氧基官能团的萘磺酰胺衍生物,并测定了它们的杀虫活性。其中一些表现出出色的活性,LC 50值低至0.202 mg ml -1,远低于阳性对照celangulin V (23.9 mg ml -1 )。此外,还讨论了构效关系,并通过分子对接验证了化合物与靶受体的结合方式。