有效合成和评估含有2-arylchromen-4-ones的的治疗潜力
Nadezhda Troshkova1, Larisa Politanskaya2, Jiaying Wang1,3
1Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of Russian Academy of Sciences, Ac. Lavrentiev Avenue, 9, Novosibirsk, 630090, Russian Federation.
Molecular diversity
|July 16, 2024
概括
这项研究合成了新型化2-arylchromen-4-ones. 一些化合物对A型流感病毒表现出显著的抗病毒活性,显示出新疗法开发的前景.
科学领域:
- 药用化学 医学化学
- 有机合成 有机合成
- 病毒学 病毒学
背景情况:
- 2 - 亚利克罗门-4 - 是一种具有多种生物活性的异环化合物.
- 的结合可以调节有机分子的药理特性.
- 流感A型病毒仍然是一个重大的全球健康问题,需要新的抗病毒药物.
研究的目的:
- 为了合成一系列新的化2-arylchromen-4-one衍生物.
- 为了评估合成的化合物对细胞毒性,抗糖化,酶抑制 (胆酶,碳酸酶),抗氧化活性和抗病毒作用.
- 为了确定有前途的候选人进一步药物开发.
主要方法:
- 通过化2-基亚基和甲的凝结合成,然后在DMSO中使用I2进行2'-基基的氧化循环.
- 使用质母细胞瘤 (SNB19) 和正常 (Vero) 细胞系进行细胞毒性评估.
- 抗糖化活性评估.
- 酶抑制测定用于乙胆酶,丁胆酶和氧胆酶.
- 使用ABTS和FRAP测试来确定抗氧化剂活性.
- 在MDCK细胞培养中对流感A病毒 (H1N1) 进行抗病毒查.
主要成果:
- 一系列化2 - 烯基-4-子被成功合成.
- 化合物32,31和39对高选择性指数 (SI=57,38和25分别) 的流感A病毒 (H1N1) 具有显著的抗病毒活性.
- 一些化合物显示中度抗糖化,酶抑制和抗氧化活性.
结论:
- 合成的化二甲基-4-子代表了一类有前途的化合物,具有潜在的抗病毒应用.
- 化合物32,31和39需要进一步调查,因为它们是流感A病毒治疗的主要候选物.
- 这项研究强调了在设计新的生物活性异环环中加入的实用性.
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