研究新型苯乙烯基喹唑啉类似物的生物活性谱。
Investigating biological activity spectrum for novel styrylquinazoline analogues.
机构信息
Zentiva k.s., U kabelovny 130, 102 37 Prague 10, Czech Republic.
出版信息
Molecules. 2009 Oct 23;14(10):4246-65. doi: 10.3390/molecules14104246.
Abstract
In this study, series of ring-substituted 2-styrylquinazolin-4(3H)-one and 4-chloro-2-styrylquinazoline derivatives were prepared. The syntheses of the discussed compounds are presented. The compounds were analyzed by RP-HPLC to determine lipophilicity. They were tested for their inhibitory activity on photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Primary in vitro screening of the synthesized compounds was also performed against four mycobacterial strains and against eight fungal strains. Several compounds showed biological activity comparable with or higher than that of the standard isoniazid. It was found that the electronic properties of the R substituent, and not the total lipophilicity of the compound, were decisive for the photosynthesis-inhibiting activity of tested compounds.
摘要
在这项研究中，我们制备了一系列环取代的 2-苯乙烯基喹唑啉-4(3H)-酮和 4-氯-2-苯乙烯基喹唑啉衍生物。介绍了所讨论化合物的合成方法。通过反相高效液相色谱法（RP-HPLC）分析这些化合物以确定其亲脂性。并测试了它们对菠菜（Spinacia oleracea L.）叶绿体光合作用电子传递（PET）的抑制活性。还对合成的化合物进行了初步的体外筛选，以对抗四种分枝杆菌菌株和八种真菌菌株。一些化合物显示出与标准异烟肼相当或更高的生物活性。研究发现，R 取代基的电子性质，而不是化合物的总亲脂性，是测试化合物抑制光合作用活性的决定性因素。
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