设计,合成和各种生物活性含有乙基的母体类似物
Wanjun Ni1, Hongjian Song1, Lizhong Wang1
1State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, College of Chemistry, Frontiers Science Center for New Organic Matter, Nankai University, Tianjin 300071, China.
含有乙基片段的新型母体衍生物对烟草马赛克病毒 (TMV) 具有强烈的抗病毒活性. 一些化合物还表现出显著的杀虫性能,表明这些新型化合物的广泛生物应用.
科学领域:
- 药用化学 医学化学
- 自然产品化学 自然产品化学
- 农业化学 农业化学
背景情况:
- 含有乙基的化合物由于其电子捐赠/接受特性,具有显著的生物活性.
- 马特林是一种天然类化合物,可以作为开发新生物活性分子的支架.
- 修改天然产品可以提高其有效性并扩大其应用.
研究的目的:
- 通过在C-14或C-11位置引入酸片段来合成新的酸衍生物.
- 评估这些衍生品对烟草马赛克病毒 (TMV) 的抗病毒活性.
- 评估合成化合物的杀虫剂和杀真菌活性.
主要方法:
- 合成14-酸和11-丁酸的母性衍生物.
- 对TMV抗病毒活性的生物测试,与利巴维林和宁南辛进行比较.
- 对钻石背和蚊子幼虫的杀虫活性评估.
- 杀菌活性的评估.
主要成果:
- 许多合成的母体衍生物显示出出色的抗TMV活性.
- 在25种14-酸衍生物中的17种和20种11-酸衍生物中的17种显示出比利巴维林更高的TMV抑制.
- 一种特定的N-基-11-butanhydrazone衍生物表现出优越的抗TMV活性,优于Ningnanmycin.
- 几种化合物显示出对Plutella xylostella和Culex pipiens pallens的强烈杀虫活性.
结论:
- 修改matrine的乙化是一种有效的策略,用于开发针对TMV的强效抗病毒药物.
- 合成的化合物显示出作为具有抗病毒和杀虫功能的广谱农业化学品的前景.
- 对化合物的进一步研究是有必要的,因为它具有作为一种新型抗病毒药物的潜力.
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