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以蚕沙叶绿素稳定降解产物二氢卟吩f(2)为关键中间体,设计合成了2-(1-羟基)乙基二氢卟吩f(3a)3及其醚类衍生物3b-3d、4b-4d,其中,3a.4c.4d为新化合物,用UV.IR.^1HNMR和FAB-MS确证了它们的结构。同时测定了目标物3a.4b-4d对小鼠肉瘤-180移植瘤的光动力治疗作用,结果显示:2-(1-羟基)乙基二氢卟吩f醚衍生物4b-4d对小鼠肉瘤-180移植瘤的光动力治疗效果均优于参比药物血卟啉生物(HpD),且随醚链增长而增强,而3a却无效,这将对进一步的构效关系研究具有重要的意义。  相似文献
2.
光学纯羟基醚类化合物的合成和分离   总被引:1,自引:0,他引:1  
dl-羟基醚类化合物3-奎宁环基-2’,2’,2’-苯基环戊基羟基乙基醚Ⅰ的抗胆碱作用已有报道。  相似文献
3.
A series of lamiridosin A derivatives were synthesized through simple procedures. Their antitumor activities were evaluated against EC9706, MGC803, and B16 cell lines in vitro. Several compounds showed potent antitumor activity, especially compound 10, with IC50 value of 2.36 μmol/L against MGC803 cell lines, is more potent than marketed positive drug 5-fluorouridine (5-FU).  相似文献
4.
目的 基于前期研究表明二氢卟吩f的3-乙烯基成醚修饰具有更强的光敏抗肿瘤活性而设计合成二氢卟吩p6醚类光敏剂(1),研究其初步体外光动力抗癌活性。方法 以蚕沙叶绿素a粗提物酸水解产物脱镁叶绿酸a(5)经碱及空气氧化降解制得的紫红素-18(4)为先导物,通过碱水解和CH2N2甲基化制得二氢卟吩p6三甲酯(2),2与33% HBr加成后再和烷氧醇发生亲核取代反应生成目标化合物(1),并评价其对黑色素瘤B16-F10细胞的光动力杀伤效应。结果 6个目标化合物1a-1f对黑色素瘤B16-F10细胞的体外光动力抗癌活性均优于同类阳性对照药他拉泊芬和维替泊芬,其结构经电喷雾质谱(ESI-MS)、氢谱(1H NMR)、碳谱(13C NMR)及电喷雾高分辨质谱(ESI-HRMS)确证。结论 二氢卟吩p6醚类光敏剂具有光动力抗癌活性强、治疗指数(暗毒/光毒比)高等优点,值得进一步开发研究。  相似文献
5.
A new lipidic acid-amido ether derivative (LAAE-14) able to reduce dose-dependently the calcium increases mediated either by calcium ionophore ionomycin, by the endoplasmic reticular Ca(2+)-ATPase inhibitor thapsigargin, or by the chemotactic tripeptide N-formyl-L-methionyl-L-leucyl-L-phenylalanine (fMLP), in human neutrophils as well as in murine peritoneal macrophages, but not ATP, has been evaluated as a potential anti-inflammatory drug. This compound attenuated leukocyte activation by means of its inhibitory effect on the respiratory burst elicited in both types of cells by 12-O-tetradecanoyl phorbol 13-acetate, by inhibition of the degranulation process induced by cytochalasin B+fMLP or cytochalasin B+platelet activating factor, as well as by reduction of leukotriene B(4) synthesis induced by the calcium ionophore A23187. In addition, in zymosan-stimulated mouse peritoneal macrophages LAAE-14 caused a potent inhibition of nitrite and prostaglandin E(2) production. This compound exerted acute and chronic anti-inflammatory effects by oral route, that may be related with several mechanisms such as attenuation of leukocyte activation, inhibition of inducible nitric oxide synthase, cyclo-oxygenase-2 and cytosolic phospholipase A(2) expression as well as reduction in tumour necrosis factor-alpha production. Its anti-inflammatory profile is clearly correlated with its behavior as inhibitor of intracellular calcium mobilization. The profile and potency of this compound may have relevance for the inhibition of the inflammatory response at different levels and may represent a new approach to the development of new anti-inflammatory drugs.  相似文献
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应用二芳基碘鎓离子氟硼酸盐合成了 2个新的二苯醚类化合物。该方法简便易行 ,收率高 ,质量好 ,适合于多取代结构较复杂的二苯醚类化合物的合成  相似文献
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设计并合成了13 个未见文献报道的叔丁基苯哌嗪取代硫醚类目标化合物,并经元素分析、核磁共振氢谱及红外光谱确证其化学结构.对部分目标化合物进行了抗变态和抗炎等生物活性测定.结果表明:W01 ,W03 ,W07 和W09 具有较强的抗变态活性  相似文献
8.
Liquid chromatography combined with evaporative light scattering detection is a powerful tool for analyzing polymeric excipients used in pharmaceutical formulations. A versatile, gradient elution liquid chromatographic method utilizing evaporative light scattering detection (ELSD) has been developed for analyzing several types of cellulose ether and ester derivatives in pharmaceutical formulations. This single method was proven to be capable of differentiating six types of cellulose ether and ester derivatives. The influence of ELSD instrument parameters on the detector response and sensitivity has been studied by a statistical design of experiments. It was found that lowering gas flow rate increased peak area response significantly. Increasing nebulizer temperature also increased peak area response. In contrast, evaporator temperature has very minor impact on peak area response, but had a significant impact on noise level. Thus, signal to noise ratio was significantly lower for low evaporator temperature setting. Despite the logarithmic relationship between peak area responses versus concentrations, sufficient selectivity, precision and accuracy were achieved. The method has been validated for assaying hypromellose acetate succinate (HPMCAS) polymer in a pharmaceutical formulation.  相似文献
9.
As a part of a research program directed to the discovery of novel antidepressant agents, a series of new hetero[2,1]benzothiazepine derivatives was synthesized. Some of these compounds antagonized the ptosis and motor depression induced by tetrabenazine and were also active in the Porsolt forced swimming test.  相似文献
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