设计,合成和生物活动评估5-Aryl-cyclopenta[c]pyridine衍生物的设计,合成和生物活动评估
Jie Tan1,2, Changjiang Xu1, Dong Liu1
1Institute of Applied Chemistry, Jiangxi Academy of Sciences, Nanchang 330096, China.
Journal of agricultural and food chemistry
|January 4, 2025
概括
新的5-aryl-cyclopenta[c]pyridine衍生物被合成并测试其生物活性. 化合物4k显示出强大的抗烟草马赛克病毒 (TMV) 活性和低毒性,而其他衍生物则表现出杀虫剂和杀真菌的特性.
科学领域:
- 药用化学 医学化学
- 农业科学 农业科学
- 有机合成 有机合成
背景情况:
- 天然产品Cerbinal作为开发新型生物活性分子的主要化合物.
- 之前对环[c]胺的研究表明了潜在的生物活性,促使进一步调查.
- 农业对有效的抗病毒,杀虫剂和杀菌剂的需求推动了对新化学实体的研究.
研究的目的:
- 设计和合成基于大脑细胞的新型5-aryl-cyclopenta[c]pyridine衍生物.
- 评估对植物病毒的抗病毒活性,特别是烟草马赛克病毒 (TMV).
- 评估合成化合物的杀虫剂和杀菌剂特性.
主要方法:
- 通过氨基化,化和交叉合反应合成30种新型的5-aryl-cyclopenta[c]pyridine衍生物.
- 生物活性查,包括抗TMV测定 (无活化,治愈,保护作用) 和斑马鱼的毒理评估.
- 分子对接研究以了解与TMV受体蛋白的结合相互作用.
- 对昆虫杀虫活性评价Plutella xylostella和对Sclerotinia sclerotiorum,Botrytis cinerea和Phytophthora infestans的杀菌活性.
主要成果:
- 与化合物和利巴维林相比,4g和4k化合物表现出较高的抗TMV活性.
- 化合物4k在体内表现出强大的抗TMV作用和对斑马鱼的低毒性.
- 分子对接表明,环相互作用增强了与TMV受体的结合亲和力.
- 几种衍生品显示出显著的杀虫效果和广泛的杀菌活性,其中化合物4i对Sclerotinia sclerotiorum特别有效.
结论:
- 合成的5-aryl-cyclopenta[c]pyridine衍生物代表了农业应用的一类有前途的化合物.
- 化合物4k是针对TMV的抗病毒应用的潜在候选者.
- 像化合物4i这样的衍生物显示出作为有效的杀菌剂的潜力,而其他衍生物则具有杀虫剂特性,突出显示了它们的广泛用途.
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