共查询到19条相似文献,搜索用时 46 毫秒
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天然产物中先导化合物的发现与优化 总被引:4,自引:0,他引:4
本文对从天然产物中发现先导化合物的思路及先导化合物的优化方法作了简单论述。指出从天然产物中发现有活性的化合物,将仍然是先导物发现甚至是创制药物的重要组成部分。 相似文献
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天然产物与药物的发现 总被引:1,自引:0,他引:1
目前使用的的很多药物都直接或间接来自天然产物,天然产物形成了新药开发的广泛的物质上来在抗癌,抗感染,抗疟,神经系统,心血和系统和免疫系统药物领域中开发出或正在开发的有重大治疗价值的植物药充分证实了这一点。 相似文献
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天然产物在抗爱滋病病毒中研究新进展 总被引:5,自引:0,他引:5
爱滋病 ,英文名为AcquiredImmunodeficiencysynelrome ,简称AIDS。人获得性免疫缺陷病毒 (HumanImmunodefi ciencyvirus,HIV)感染是引起爱滋病的直接原因 ,它是一种逆转录病毒 ,具有复杂的生活周期。由于其怪异的病理及传染性 ,目前临床上尚无理想的治疗药物。众多的医学、药学及化学工作者正努力从各个方面寻找有效的抗爱滋病病毒的方法 ,各国研究工作者也研制出了许多对HIV有抑制作用的药物 ,比如Rajni等人[1 ] 和Tanaka等人[2 ] 合成的HEPT类化合物 ,他们能在HIV的不同生活周期中发挥作用 ,但对机体有很大的毒性 ,还不尽人意。… 相似文献
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Antimutagenic agents from natural products. 总被引:7,自引:0,他引:7
M E Wall 《Journal of natural products》1992,55(11):1561-1568
Certain secondary metabolites found in terrestrial and marine plants and organisms have evinced the capability for inhibiting the mutagenicity toward Salmonella typhimurium of a number of mutagens. These include 2-aminoanthracene (2AN), ethylmethanesulfonate (EMS), and benzo-[a]pyrene(B[alpha]P). The sensitivity of the antimutagenicity assay is such that crude extracts can be evaluated and purification of extracts readily followed. Major classes of antimutagenic compounds that have been isolated include flavonoids, coumarins, and cymopols. 相似文献
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Bioactive marine natural products, with emphasis on handling of water-soluble compounds 总被引:3,自引:0,他引:3
Y Shimizu 《Journal of natural products》1985,48(2):223-235
Recent progress in separation techniques has enabled us to work with water-soluble components which, more often than not, are responsible for biological activities found in marine organisms. Isolation techniques and chemical and biological aspects of water-soluble marine natural products will be discussed with some representative examples. 相似文献
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Marine natural products and related compounds in clinical and advanced preclinical trials 总被引:27,自引:0,他引:27
The marine environment has proven to be a very rich source of extremely potent compounds that have demonstrated significant activities in antitumor, antiinflammatory, analgesia, immunomodulation, allergy, and anti-viral assays. Although the case can and has been made that the nucleosides such as Ara-A and Ara-C are derived from knowledge gained from investigations of bioactive marine nucleosides, no drug directly from marine sources (whether isolated or by total synthesis) has yet made it to the commercial sector in any disease. However, as shown in this review, there are now significant numbers of very interesting molecules that have come from marine sources, or have been synthesized as a result of knowledge gained from a prototypical compound, that are either in or approaching Phase II/III clinical trials in cancer, analgesia, allergy, and cognitive diseases. A substantial number of other potential agents are following in their wake in preclinical trials in these and in other diseases. 相似文献
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天然产物及其衍生物中的芳香化酶抑制剂 总被引:1,自引:0,他引:1
芳香化酶是药物预防及治疗乳腺癌等雌激素依赖性疾病的一个重要靶点。综述近10年来,从天然产物及其衍生物中发现的具有芳香化酶抑制活性的化合物,通过对其化学结构、生物活性进行总结,并探讨构效关系,为新型芳香化酶抑制剂的研发提供参考。 相似文献
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Marine natural products: pyrrololactams from several sponges 总被引:4,自引:0,他引:4
Two pyrrololactams, likely degradation products of more complex known guanidines, were isolated from several marine sponges. 5-Bromo- and 4,5-dibromopyrrole-1-carboxylic acid methyl esters were also isolated. A complex guanidine metabolite, poorly soluble in DMSO, was found to give sharp, reproducible nmr spectra in acid media. 相似文献
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具有杀灭钉螺活性的植物源天然产物研究进展 总被引:1,自引:0,他引:1
钉螺(oncomelania)是日本血吸虫Schistosoma japonicum的唯一中间寄主,是血吸虫病传播过程中不可缺少的环节。目前用于杀灭钉螺的化学药物存在生产成本高、严重污染环境、钉螺耐药性和对非靶体生物的毒性等诸多问题,这使人们将研究兴趣转向从植物中寻找天然灭螺药物。从结构类型、作用机制和构效关系等方面入手,对具有杀灭钉螺活性的植物源天然产物进行归纳总结,以期为新型植物源灭螺剂的开发提供参考。 相似文献
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拓扑异构酶(topoisomerase,topo)是解决DNA复制、转录等过程中出现拓扑问题的关键酶,是抗肿瘤药物作用的重要靶点之一.天然产物是topo抑制剂的重要来源,从天然产物中发现开发topo抑制剂是抗肿瘤药物研究的热点.以天然产物结构类型,分类综述了天然存在的具有topo抑制活性的天然产物及以它们为基础改造获得... 相似文献