College of Basic Science, Tianjin Agricultural University, Tianjin 300384, China.
State Key Laboratory of Elemento-Organic Chemistry, College of Chemistry, Frontiers Science Center for New Organic Matter, Nankai University, Tianjin 300071, China.
Molecules. 2022 Oct 8;27(19):6700. doi: 10.3390/molecules27196700.
Based on the scaffolds widely used in drug design, a series of novel tryptophan derivatives containing azepine and acylhydrazone moieties have been designed, synthesized, characterized, and evaluated for their biological activities. The bioassay results showed that the target compounds possessed moderate to good antiviral activities against the tobacco mosaic virus (TMV), among which compounds , , , , , and exhibited higher inactivation, curative, and protection activities in vivo than that of ribavirin (40 ± 1, 37 ± 1, 39 ± 2% at 500 mg/L). Especially, showed comparable activities to that of ningnanmycin (57 ± 2, 55 ± 3, 58 ± 1% at 500 mg/L). Meanwhile, we were pleased to find that almost all these derivatives showed good larvicidal activities against . Meanwhile, these derivatives also showed a broad spectrum of fungicidal activities.
基于在药物设计中广泛使用的支架，设计、合成、表征并评估了一系列含有氮杂环庚烷和酰腙部分的新型色氨酸衍生物，以评估其生物活性。生物测定结果表明，目标化合物对烟草花叶病毒（TMV）具有中等至良好的抗病毒活性，其中化合物 、 、 、 、 和 在体内具有比利巴韦林更高的失活、治疗和保护活性（在 500mg/L 时分别为 40 ± 1、37 ± 1、39 ± 2%）。特别是 ，其活性与宁南霉素（57 ± 2、55 ± 3、58 ± 1%，在 500mg/L 时）相当。同时，我们很高兴地发现，几乎所有这些衍生物对 都表现出良好的杀幼虫活性。同时，这些衍生物还表现出广谱的杀菌活性。
