本文選題：長鏈烴基水楊酸　切入點(diǎn)：滅螺活性　出處：《復(fù)旦大學(xué)》2014年碩士論文　論文類型：學(xué)位論文

【摘要】：由日本血吸蟲導(dǎo)致的人畜共患血吸蟲病是我國一種常見的慢性消耗性疾病。釘螺(Oncomelania hupensis)是血吸蟲病傳播途徑的主要中間宿主,其地理分布與日本血吸蟲病一致,因此消滅釘螺是防治血吸蟲病的重要措施之一。氯硝柳胺是wHO唯一推薦商業(yè)應(yīng)用的殺螺劑,但帶來的對(duì)水生生物的毒性及對(duì)環(huán)境的影響是其主要問題。近年來對(duì)新型滅螺劑的研究更多的集中在來自植物的環(huán)境友好具有滅螺活性的成分及其合成的衍生物上。銀杏酸是銀杏葉及外種皮的主要成分,具有較強(qiáng)的殺滅釘螺活性,且具有開發(fā)成高效、低毒、價(jià)廉的新型滅螺藥物的潛力。在本課題組前期研究的基礎(chǔ)上,本實(shí)驗(yàn)從4-及5-甲基水楊酸出發(fā),共合成了18個(gè)碳鏈長度為7-13的長鏈烴基水楊酸類衍生物,包括Z式、E式以及飽和側(cè)鏈。同時(shí)在這基礎(chǔ)上,以長鏈烷基水楊酸為原料合成了14個(gè)長鏈烷基水楊酰胺類化合物。并分別根據(jù)波譜數(shù)據(jù)確定了這些化合物的結(jié)構(gòu)。對(duì)合成的長鏈烴基水楊酸和長鏈烷基水楊酰胺進(jìn)行了滅螺活性的研究發(fā)現(xiàn),長鏈烴基水楊酸的碳鏈長度對(duì)活性的影響要比取代位置更大,其滅螺活性隨著鏈長的增長而增強(qiáng),且以碳鏈長度為13個(gè)碳原子的活性為最好,長鏈中雙鍵為反式的化合物的活性與對(duì)應(yīng)的飽和長鏈化合物活性相當(dāng),且都比順式強(qiáng)；長鏈烷基水楊酰胺滅螺活性比對(duì)應(yīng)的長鏈烷基水楊酸好,同樣也以碳鏈長度為13的酰胺類化合物活性為最好。急性魚毒性實(shí)驗(yàn)結(jié)果顯示長鏈烷基水楊酸化合物對(duì)魚的毒性濃度遠(yuǎn)高于對(duì)釘螺的殺傷濃度,與氯硝柳胺相比,毒性更低,說明了這類化合物在實(shí)際應(yīng)用中要比氯硝柳胺安全。
[Abstract]:Zoonotic schistosomiasis caused by Schistosoma japonicum is a common chronic and expendable disease in China. Oncomelania hupensis is the main intermediate host of schistosomiasis transmission and its geographical distribution is consistent with that of schistosomiasis japonicum. Therefore, the elimination of snail is one of the important measures to control schistosomiasis. Niclosamide is the only snail killer recommended for commercial use by wHO. However, the toxicity to aquatic organisms and the impact on the environment are the main problems. In recent years, the research on new snail repellents has focused more on the environmentally friendly components with snail killing activity from plants and their synthetic derivatives. Ginkgolic acid is the main component of ginkgo biloba leaves and exocarps. It has the potential to develop new snail killing drugs with high efficiency, low toxicity and low price. Based on the previous research of our group, the experiment starts from 4- and 5-methylsalicylic acid. A total of 18 long-chain alkyl salicylic acid derivatives with a length of 7-13 carbon chains were synthesized, including Z type E and saturated side chains. Fourteen long chain alkyl salicylic amides were synthesized from long chain alkyl salicylic acid. The structures of these compounds were determined based on the spectral data. The synthesis of long chain alkyl salicylic acid and long chain alkyl salicylidene amide were studied. The activity of snail killing was studied. The carbon chain length of long chain alkyl salicylic acid has more influence on the activity than the substitution position. The snail killing activity increases with the increase of chain length, and the carbon chain length of 13 carbon atoms is the best. The activity of the double bond trans compounds in the long chain is equal to that of the corresponding saturated long chain compounds, and the activity of the long chain alkyl salicylic amide is better than that of the corresponding long chain alkyl salicylic acid, and the activity of the long chain alkyl salicyamide is better than the corresponding long chain alkyl salicylic acid. The results of acute fish toxicity test showed that the toxicity concentration of long chain alkyl salicylic acid compounds to fish was much higher than the killing concentration of Oncomelania hupensis, and the toxicity was lower than that of niclosamide. It shows that this kind of compound is safer than niclosamide in practical application.
【學(xué)位授予單位】：復(fù)旦大學(xué)
【學(xué)位級(jí)別】：碩士
【學(xué)位授予年份】：2014
【分類號(hào)】：R914;R96

【參考文獻(xiàn)】

相關(guān)期刊論文 前1條

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本文編號(hào)：1652031