【摘要】：本論文在查爾酮化合物中引入具有廣泛生物活性的嘌呤環(huán),設計合成一系列含嘌呤取代的查爾酮類衍生物3a-3z,并以黃瓜花葉病毒與煙草花葉病毒為研究對象,采用半葉枯斑法對目標化合物進行活體內抗植物病毒活性測試;并對目標化合物與TMV CP之間的相互作用進行了初步探究。本論文的工作總結概括如下:1.以天然產(chǎn)物查爾酮為先導化合物,通過活性結構拼接原理,將同樣具有廣泛生物活性的嘌呤環(huán)引入查爾酮結構中,設計合成了26個新型含嘌呤取代的查爾酮衍生物3a-3z。所有的化合物均通過了1H NMR、13C NMR、HRMS和元素等結構表征。2.以寧南霉素和病毒唑(利巴韋林)作為對照藥劑,采用半葉枯斑法,測試目標化合物對黃瓜花葉病毒(CMV)和煙草花葉病毒(TMV)的抑制活性。結果表明:在濃度為500μg/mL時,大部分化合物對CMV表現(xiàn)出較好的治療活性,因此進一步測試了目標化合物抗CMV治療活性的EC50值,其中化合物3o(EC50=301.1μg/mL)、3s(EC50=315.7μg/mL)、3w(EC50=282.3μg/mL)和3x(EC50=230.5μg/m L)對CMV的治療活性優(yōu)于寧南霉素(EC50=343.8μg/mL)。在抗TMV活性方面,化合物3o和3p的表現(xiàn)出較好的鈍化活性,分別為89.1%和88.2%,與寧南霉素相當(89.5%)。3.采用熒光光譜檢測法,進一步探究部分目標化合物與TMV CP之間的相互作用,結果表明高活性化合物3o與TMV CP之間具有較強的親和力。
[Abstract]:In this paper, a series of chirone derivatives 3a-3zcontaining purine substituents were designed and synthesized by introducing a wide range of purine rings into chalcone compounds. Cucumber mosaic virus and tobacco mosaic virus were studied. The in vivo anti-virus activity of the target compound was tested by half-leaf spot method. The interaction between the target compound and TMV CP was studied. The work of this paper is summarized as follows: 1. With the natural product chalcone as the lead compound, 26 new derivatives 3a-3zwith purine substituent were designed and synthesized by introducing the purine ring, which also has extensive biological activity, into the structure of chalcone by the principle of active structure splicing. All the compounds were characterized by 1H NMR,13C NMR,HRMS and elemental structure. The inhibitory activities of the target compounds against cucumber mosaic virus (CMV) and tobacco mosaic virus (TMV) were tested by semi-leaf blight spot method with Ningnanmycin and ribavirin (ribavirin) as control agents. The results showed that at the concentration of 500 渭 g/mL, most of the compounds showed better therapeutic activity to CMV, so the EC50 value of the target compound's anti-CMV therapeutic activity was further tested, in which compound 3o (EC50=301.1 渭 g/mL), 3s (EC50=315.7 渭 g/mL), 3w (EC50=282.3 渭 g/mL) and 3x (EC50=230.5 渭 g / mL) were superior to EC50=343.8 渭 g/mL in the treatment of CMV. The anti- TMV activity of compounds 3o and 3p were 89.1% and 88.2% respectively, which were equivalent to those of Ningnanmycin (89.5%). The interaction between some target compounds and TMV CP was further investigated by fluorescence spectrometry. The results showed that the highly active compound 3o had strong affinity with TMV CP.
【學位授予單位】：貴州大學
【學位級別】：碩士
【學位授予年份】：2017
【分類號】：O621.3;TQ450.1

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