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研究川木香抗炎活性与其HPLC指纹图谱的谱效关系,探究其抗炎活性成分.采用HPLC-DAD法获取12个川木香样本水提物的指纹图谱,小鼠耳廓肿胀试验检测川木香的抗炎活性.运用偏最小二乘法进行谱效相关性分析,以标准品比对及HPLC-MS/MS法对抗炎活性贡献较大的色谱峰进行鉴定.从川木香指纹图谱中共确定了17个共有峰,川木香水提物对二甲苯所致小鼠耳廓肿胀有一定的抑制作用.谱效关联研究结果显示有10个共有峰与抗炎活性呈正相关,依次为P8>P4>P3>P10>P14>P15>P7>P5>P9>P16,其中色谱峰P3、P4、P8、P10分别鉴定为紫丁香苷、绿原酸、咖啡酸和1,3-O-二咖啡酰奎尼酸.方法可为川木香抗炎活性药效物质基础的发现及其"药效关联"的质量标准的建立提供一定的技术理论支持. 相似文献
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从毛姜花(Hedychium villosum Wall.)中分离得到1个新二萜(1)和1个已知二萜(3). 新二萜命名为Villosumcoronarin, 该化合物在氯仿或甲醇溶液中发生异构化, 部分转化为其差向异构体1'; 其平面结构经质谱、红外光谱、氢谱、碳谱及无畸变极化转移增强技术(DEPT)、氢氢相关谱(1H-1H COSY)和异核多键相关谱(HMBC)等方法确证; 其相对构型由氢谱、ROESY及量化计算确证. 化合物3用琼斯试剂氧化后得到化合物4. 生物活性筛选结果表明, 化合物1对人白血病细胞株(HL-60)和肝癌细胞株(SMMC-7721)具有强的细胞毒活性, 其活性超过阳性对照顺铂(DDP). 化合物4对HL-60和SMMC-7721细胞具有显著的细胞毒活性. 相似文献
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支链/环链烷氧基乙酸为离去配体的铂(Ⅱ)配合物的体外活性研究 总被引:1,自引:0,他引:1
合成了12个带支链/环链烷氧基乙酸为离去基团的顺铂类配合物,通过元素分析、红外光谱、核磁共振氢谱和质谱对配合物进行了表征。研究了所有化合物对人非小细胞肺癌A549、人肝癌细胞BEL-7402和人乳腺癌细胞MCF-7细胞系的体外抗肿瘤活性。测试结果表明,12个配合物中有5个对人乳腺癌细胞系MCF-7有较好的体外活性。其中化合物2(顺-二(异丙氧基乙酸根)·二氨合铂(Ⅱ))在所有的化合物中显示最高的活性,对所测3个细胞系都是如此。 相似文献
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1,2,3-噻二唑-4-乙酰胺(吗啉)类衍生物的合成与生物活性 总被引:1,自引:0,他引:1
以双乙烯酮为起始原料, 设计并合成了一系列新颖的1,2,3-噻二唑-4-乙酰苯胺(吗啉)类化合物, 通过元素分析、红外光谱、核磁共振氢谱和质谱对其结构进行了表征. 生物活性测试结果表明,部分化合物具有一定的抗TMV活性、 植物生长调节活性和杀菌活性. 相似文献
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新型不对称草酰二胺类化合物的设计、合成及生物活性 总被引:1,自引:0,他引:1
以氯虫酰胺和氟虫腈骨架结构为基础, 依据生物合理设计思想引入酰胺键活性基团, 设计合成了一系列新型不对称草酰二胺类化合物, 通过核磁共振氢谱和高分辨质谱对合成的化合物进行了结构表征. 初步生物活性测试结果表明, 在浓度为200 mg/L时, 目标化合物未表现出良好的杀粘虫活性, 但具有一定的抑菌活性; 在浓度为50 mg/L时, 化合物6e和6f对番茄早疫病菌的抑菌率为45.0%, 高于其它化合物, 表明含有2,4,6-三氯苯环的该系列化合物对番茄早疫病菌具有良好的抑菌活性; 化合物6g对苹果轮纹病菌的抑菌率为51.9%, 高于其它化合物, 表明含有较大空间位阻的该系列化合物对苹果轮纹病菌具有良好的抑菌活性. 相似文献
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Twenty novel cinnamamide derivatives were designed and synthesized using as lead compound pyrimorph, whose morpholine moiety was replaced by β-phenylethylamine. All the compounds were characterized by their spectroscopic data. The fungicidal and insecticidal activities were also evaluated. The preliminary results showed that all the title compounds had certain fungicidal activities against seven plant pathogens at a concentration of 50 μg/mL, and compounds 11a and 11l showed inhibition ratios of up to 90% against R. solani. Most of the title compounds exhibited moderate nematicidal activities. In general, the morpholine ring may be replaced by other amines and a chlorine atom in the pyridine ring is helpful to fungicidal activity. 相似文献
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本文以苯甲酸为原料,经酰氯化、酰化反应得到中间体苯甲酰基异硫氰酸酯,再与2-氨基-1,3,4-噻二唑经加成反应合成并表征了10种N-苯甲酰基-N’-1,3,4-噻二唑-2-基硫脲3a-3j。初步生物活性测试结果表明:当浓度为10 mg/L时,3a~3d对小麦生根和发芽有一定的调节活性。当浓度为100 mg/L时,大部分化合物对黄瓜灰霉病菌、黄瓜炭疽病菌、水稻纹枯病菌、水稻稻瘟病菌有明显的抑制活性,而对棉花枯萎病菌的抑制活性较差。目标化合物的取代基会影响其生长调节活性和抑菌活性。结合量化计算结果讨论了化合物结构对抑菌活性的影响。 相似文献
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通过活性亚结构拼接的方法, 设计合成了一系列含四取代苯基的吡唑-4-甲酰胺类化合物, 所有化合物的结构均通过高分辨质谱(HRMS)和核磁共振氢谱(1H NMR)确证. 生物活性测试结果表明, 部分化合物对苹果纹轮病菌、 水稻纹枯病菌、 油菜菌核病菌和黄瓜灰霉病菌表现出较好的杀菌活性. 化合物5c表现出较广的杀菌谱, 在浓度为50 μg/mL时对苹果纹轮病菌的抑制活性高达95.5%. 初步构效关系分析发现, 吡唑环N取代基为甲基或叔丁基时, 化合物表现出较好的活性; 含并环结构的化合物5′杀菌活性低于含单个苯环的化合 物5; 苯环取代基R2为低于4个碳的脂肪链时, 化合物杀菌活性更高. 相似文献
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Three series of novel sulfonylureas (SUs) 9-11 containing aromatic-substituted pyrimidines were designed and synthesized. The 3D-QASR and molecular docking studies showed that SUs should be considered as potential antiphytopathogenic fungal agents. 相似文献
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A number of novel strobilurin analogues containing substituted N-phenylpyrimidin-2-amines were synthesized.The structures of these new compounds were confirmed by ~1H NMR,IR and elemental analysis.Biological evaluation in the greenhouse showed several compounds have good fungicidal activities at 25 mg/L. 相似文献
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Acetohydroxyacid synthase(AHAS) was considered as a promising target for antifungal agents.Herein,three series of novel sulfonylureas(SUs) 9-11 containing aromatic-substituted pyrimidines were designed and synthesized according to pharmacophore-combination and bioisosterism strategy.The in vitro fungicidal activities against ten phytopathogenic fungi indicated that most of the title compounds exhibited broad-spectrum and excellent fungicidal activities.Based on the preliminary fungicidal activities,a CoMFA model was constructed and the 3 D-QSAR analysis indicated that either a bulky group around the 5-position of the pyrimidine ring or electropositive group around the 2-position of the benzene ring would be favour to fungicidal activities.In order to study interaction mechanism,10 k was automatically docked into yeast AHAS and it further indicated that bearing bulky groups-aryl at the pyrimidine ring was critical to enhance antifungal activities.It revealed that the antifungal activity of derivatives 9-11 probably results from the inhibition of fungal AHAS.Thus,the present results strongly showed that SUs should be considered as lead compounds or model molecules to develop novel antiphyt o pathogenic fungal agents. 相似文献
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In a search for novel agrochemical with high activity and low toxicity, a series of substituted 4,5-dihydro-imidazol-5-one containing selenomorpholine group were synthesized by a three-step synthetic route starting from 2-azido-3-aryl-acrylic acid ethyl ester. The structures of title compounds were confirmed by ^1H NMR, IR, mass spectroscopy and elemental analysis. The preliminary bioassay against GibbereUa zeae, Fusarium oxysporum, Pellicularia sasakii, Physalospora piricola and Cercospora beticola indicated that most title compounds displayed fungicidal activity at the concentration of 50 ppm and compounds 41,4n, 40 were found to have particularly high activities against Physalospora piricola. A further in vivo test showed that compounds 41, 4n and 4o possessed better fungicidal activity against Physalospora piricola at a concentration of 100 ppm than Carbendazim. To our knowledge, this is first report that 4,5-dihy-dro-imidazol-5-one containing selenomorpholine group display fungicidal activity against Physalospora piricola. 相似文献