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吡啶并[2,3-d]嘧啶类化合物及其氧代衍生物具有潜在的生物学和药理学活性,治疗领域广泛。主要阐述了-种吡啶并[2,3-d]嘧啶类化合物医药中间体的获得方法,该法以乙氧基甲叉丙二酸二乙酯、S-甲基异硫脲硫酸盐为起始原料,通过6步反应合成目标化合物8-甲基-2-甲硫基-8氢-吡啶并[2,3-d]嘧啶-7-酮,收率稳定可靠。 相似文献
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Roscovtine是人工合成的嘌呤类CDK抑制剂,已进入抗肿瘤临床研究阶段。Roscovitine的发现使得许多研究团队开始关注这类结构,并在此基础上进行了大量的结构优化。已经报道的嘌呤类CDK抑制剂中,仅有6类结构以Roscovitine作为对照进行生物活性研究。其中,吡唑并[1,5-a]-1,3,5-三嗪类、吡唑并[1,5-a]嘧啶类、吡唑并[1,5-a]吡啶类和吡唑并[4,3-d]嘧啶类在生物活性方面有所提高。对这一系列CDK抑制剂的研究进展进行综述,为新型CDK抑制剂的研究提供帮助。 相似文献
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《广西中医药大学学报》2010,(3)
[目的]研究邻菲咯啉衍生物的合成方法及衍生物的抗癌活性。[方法]以邻菲咯啉为原料合成邻菲咯啉衍生物,用质谱、核磁共振表征了其结构,并用MTT法对其进行了抗肿瘤活性初步研究。[结果]合成得到5个邻菲咯啉衍生物:2-(1H-苯并咪唑-2-基)-1,10-邻菲咯啉(化合物1)、2-(1H-萘并[2,3-d]咪唑-2-基)-1,10-邻菲咯啉(化合物2)、2-(5,6-二苯基-1,2,4-三唑-3-基)-1,10-邻菲咯啉(化合物3)、9-(1,10-邻菲咯啉-2-基)萘[1,2-e][1,2,4]三嗪(化合物4)、3-(1,10-邻菲咯啉-2-基)菲咯啉基[9,10-e][1,2,4]三嗪(化合物5)。其中化合物2-(1H-苯并咪唑-2-基)-1,10-邻菲咯啉以及2-(1H-萘并[2,3-d]咪唑-2-基)-1,10-邻菲咯啉浓度为20μg/ml时,对人胃癌细胞株SGC7901体外有一定抑制作用。[结论]邻菲咯啉衍生物的合成,可为开发高效、低毒的抗肿瘤药物提供科学依据。 相似文献
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目的设计合成2,3,3a,4-四氢硫色烯并[4,3-c]吡唑类化合物,并对其抗真菌活性进行初步评价。方法以取代苯硫酚为起始原料,首先合成中间体3-次苄基硫色满酮;然后利用水合肼和3-次苄基硫色满酮在醋酸中反应生成目标化合物。采用二倍稀释法对目标化合物的体外抗真菌活性进行测试。结果共合成了8个新的2,3,3a,4-四氢硫色烯并[4,3-c]吡唑类化合物,并经过H-核磁共振、质谱和元素分析等确认了其结构。抗真菌活性实验结果表明,目标化合物对大部分供试真菌具有好的活性。结论2,3,3a,4-四氢硫色烯并[4,3-c]吡唑类化合物在体外具有抗真菌活性,有待深入研究。 相似文献
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小花鬼针草中咖啡酰奎宁酸类成分及其抑制组胺释放活性 总被引:2,自引:0,他引:2
目的研究小花鬼针草B id ens p arv if lora全株的化学成分,并通过抑制组胺释放活性方法寻找生物活性化合物。方法采用硅胶、Sephadex LH-20和ODS柱色谱分离化合物,运用1D NM R,2D NM R等波谱法鉴定了化学结构,通过组胺抑制实验探讨抗炎活性。结果分离鉴定6种咖啡酰奎宁酸类化合物及其甲酯,分别是3,5-二氧咖啡酰奎宁酸(3,5-d i-O-caffeoy lqu in ic ac id,Ⅰ)、3,4-二氧咖啡酰奎宁酸(3,4-d i-O-caffeoy lqu in ic ac id,Ⅱ)、4,5-二氧咖啡酰奎宁酸(4,5-d i-O-caffeoy lqu in ic ac id,Ⅲ)、4-氧-咖啡酰奎宁酸(4-O-caffeoy lqu in ic ac id,Ⅳ)、5-氧-咖啡酰奎宁酸(5-O-caffeoy lqu in ic ac id,Ⅴ)、4-[3-(3,4-二羟基苯基)-丙烯酰氧基]-2,3-二羟基-2-甲基-丁酸{4-[3-(3,4-d ihydroxy-pheny l)-acry loy loxy]-2,3-d ihydroxy-2-m ethy l-bu tyric ac id,Ⅵ}。结论所有化合物均为首次从该植物中分得,化合物Ⅵ为新化合物。这些化合物显示一定的抑制组织胺释放活性。 相似文献
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灯盏乙素衍生物的合成及抗大鼠心肌缺血活性研究 总被引:2,自引:1,他引:1
[目的]设计合成一系列灯盏乙素衍生物并测试其保护大鼠缺血性心肌细胞活性,并初步探讨构效关系。[方法]以灯盏乙素为原料,将其水解后与卤代烷反应合成一系列灯盏乙素苷元的醚类衍生物;采用噻唑蓝(MTT)法测试化合物对缺氧损伤大鼠心肌细胞的保护作用。[结果]合成3个中间体及13个目标化合物,其中化合物2、4、5对缺氧损伤大鼠心肌细胞保护作用强于阳性对照药。[结论]灯盏乙素结构中糖基的有无对活性影响不大;4’位羟基为保护缺血大鼠心肌细胞的活性必须基团。 相似文献
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杜仲是我国传统的名贵药材,有补肝降压、增强免疫功能及抗癌、抗疲劳等多种药理作用[1,2]。药理研究表明,杜仲中的京尼平苷、京尼平苷酸等环烯醚萜类化合物是主要的降血压活性成分,而其中的桃叶珊瑚苷却具有升高血压的作用[3,4]。因此,将杜仲中京尼平苷、京尼平苷酸与桃叶珊瑚苷分离十分有应用价值。固相萃取技术是一个包含液相和固相的物理过程,在药物、环境、农药等的分析中常作为一种预处理手段,具有分离纯化效率高、操作简便、溶剂耗量少等优点[5]。本实验采用以未键合的硅胶为填料进行固相萃取,以不同极性的溶剂萃取分离纯化杜仲中的环… 相似文献
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甘草酸、甘草次酸衍生物的合成及生物活性研究进展 总被引:1,自引:0,他引:1
甘草酸、甘草次酸是甘草中最重要的活性成分,具有广泛的生物活性,尤其是其衍生物具有显著的抗炎、抗乙肝病毒、抗艾滋病毒等活性。近年来国内外专家合成了许多结构各异的甘草酸、甘草次酸衍生物,并研究了其相关的药理活性。文章综述了近年国内外对甘草酸、甘草次酸衍生物合成及活性研究所取得的新进展。 相似文献
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吩噻嗪是含杂原子的三环化合物,于19世纪后半叶在染料工业中发现并被应用。近年来,陆续发现以吩噻嗪结构为母核的部分衍生物具有抗癌、抗菌、抗阿尔兹海默症、抗氧化以及抗病毒等多种药理活性。笔者综述了吩噻嗪类化合物的合成及其相关生物活性研究进展,总结不同活性类型吩噻嗪衍生物的构效关系,为吩噻嗪类化合物的深入系统研究提供参考。 相似文献
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青蒿素类化合物具有独特的过氧桥结构,对恶性疟疾具有显著的治疗作用,且不易产生耐药性。青蒿素及其衍生物还具有抗血吸虫病、抗肿瘤、抗菌、抗炎、抗病毒、抗纤维化等药理作用。确定了青蒿素的结构,并对其生物合成、化学合成及结构改造进行一系列研究。结构改造得到的双氢青蒿素、青蒿琥酯、蒿甲醚等化合物,有效改善了青蒿素的理化性质和成药性,目前已有复方双氢青蒿素、复方青蒿素、复方蒿甲醚等制剂应用于临床。对近年来青蒿素及其衍生物的结构改造、药理作用、临床应用、安全性、专利申请及保护等的研究进展进行综述,以期为青蒿素及其衍生物的进一步开发利用提供参考。 相似文献
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Xanthone and its derivatives occupy a large part of the family of natural polyphenolic compounds with various biological and pharmacological activities.In recent years(from 2006 to 2011),it was reported that 127 xanthones were discovered from plants and fungi using various modern separation methods including silica gel/polyamide column chromatography,HPLC,high-speed counter-current chromatography,high-performance centrifugal partition chromatography,etc.Since total synthesis and structure modification for xanthone and its derivatives have been given attention worldwide,we introduced the synthetic methods of xanthone skeletons as well.Unfortunately,to date,there are still weaknesses in current methods of separation and synthesis,which need to be improved.This review,to a certain extent,provides necessary foundation for the further research and development of medicines containing xanthone and its derivatives. 相似文献
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Expanding the Therapeutic Spectrum of Artemisinin:
Activity Against Infectious Diseases Beyond Malaria and
Novel Pharmaceutical Developments 下载免费PDF全文
Thomas Efferth Marta R. Romero Anna Rita Bili Ahmed Galal Osman Mahmoud ElSohly Michael Wink Rudolf Bauer Ikhlas Khan Maria Camilla Bergonzi Jose J.G. Marin 《World Journal of Traditional Chinese Medicine》2016,2(2)
The interest of Western medicine in Traditional Chinese Medicine(TCM) as a source of drug leads/new drugs to treat diseases without available efficient therapies has been dramatically augmented in the last decades by the extensive work and the outstanding findings achieved within this kind of medicine. The practice of TCM over thousands of years has equipped scientists with substantial experience with hundreds of plants that led to the discovery of artemisinin(qinghaosu), which is extracted from the medicinal plant Artemisia annua L.(qinghao). The unexpected success of artemisinin in combating malaria has drawn strong attention from the scientific community towards TCM. Artemisinin was discovered by Youyou Tu in 1972. Since then, several novel pharmacological activities based on the well-known properties of the sesquiterpene lactone structure with the oxepane ring and an endoperoxide bridge have been unravelled. Beyond malaria, artemisinin and its derivatives(artemisinins) exert profound activities towards other protozoans(Leishmania, Trypanosoma, amoebas, Neospora caninum, and Eimeria tenella), trematodes(Schistosoma, liver flukes), and viruses(human cytomegalovirus, hepatitis B and C viruses). Less clear is the effect against bacteria and fungi. Based on the promising results of artemisinin and the first generation derivatives(artesunate, artemether, arteether), novel drug development strategies have been pursued.These included the synthesis of acetal-and non-acetal-type artemisinin dimeric molecules as well as developing nanotechnological approaches, e.g.artemisinin-based liposomes, niosomes, micelles, solid lipid nanocarriers, nanostructured lipid carriers, nanoparticles, fullerenes and nanotubes. The current review presents an overview on different aspects of artemisinins, including sources, chemistry, biological/pharmacological properties, types of infectious pathogens that are susceptible to artemisinins in vitro and in vivo, in addition to the advancement in their drug delivery systems utilizing pharmaceutical technology. It would be expected that different therapeutic strategies based on the second and third generation artemisinin derivatives and artemisinin-based drug technologies would be available in the near future to treat specific infectious diseases. 相似文献
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以西红花苷为代表的脱辅基类胡萝卜素类化合物是传统中药西红花Crocus sativus的主要药效成分,具有广泛的抗氧化、抗炎、抗粥样动脉硬化、抗癌、抗抑郁等药理活性。西红花中类胡萝卜素的生物合成途径包括以甲羟戊酸起始合成牻牛儿基牻牛儿基焦磷酸至玉米黄质的传统上游路径,以及裂解玉米黄质特异性合成西红花酸及西红花苷的下游途径。对近年来西红花中类胡萝卜素代谢途径相关关键酶基因的研究现状进行综述,为进一步解析合成西红花苷等类胡萝卜素衍生物的下游途径指明方向,更为后续采用代谢工程的手段提高西红花苷等药效物质产量提供理论依据。 相似文献
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??OBJECTIVE To study the synthesis and activities of AHPN derivatives. METHODS Starting from p-bromophenol and 1-adamantanol, a series of AHPN derivatives were synthesized by substitution reaction, condensation reaction, oxidation reaction and reduction reaction. These new compounds were characterized by 1H-NMR, 13CNMR and HR-MS. Biacore technique was used to test the derivatives?? combining activities with RAR??. RESULTS Four compounds, 7c, 6c, 6e, and 6h, exhibited significant combining activities with RAR?? compared with AHPN. The introduction of phosphoric acid groups and nitrogen heterocyclic ring increased the activities of these compounds. CONCLUSION Compounds 7c, 6c, 6e, and 6h show significant combining activities with RAR??, which are worthy of further study. 相似文献