共查询到19条相似文献,搜索用时 62 毫秒
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4-色满酮芳环Mannich碱类化合物的合成及其抗血小板聚集活性研究 总被引:1,自引:0,他引:1
4-色满酮类化合物和色酮类化合物具有广泛的生物活性。笔者曾发现4-色满酮3位Mannich碱类化合物具有显著的抗血小板聚集活性,为了考察在4-色满酮的3-位Mannich碱类化合物中3-位胺甲基侧链是否为加强活性的必需基团,为确定其药效构象提供信息,笔者设计合成了4种4-色满酮芳环Mannich碱类化合物,同时又合成了3种色酮芳环Mannich碱类化合物。所合成的目标化合物均未见文献报道,其组成和结构经红外光谱、质谱和核磁共振氢谱确认。采用Born's比浊法对目标化合物进行了抗血小板聚集活性的体外筛选。实验结果表明,目标化合物对ADP和胶原诱导的家兔血小板聚集均具有显著的体外抑制活性。 相似文献
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4-色满酮曼尼希碱类化合物的合成及其抗血小板聚集活性 总被引:2,自引:1,他引:1
4-色满酮类化合物具有广泛的生物活性。为了考察4-色满酮类化合物的抗血小板聚集活性构效关系,笔者设计合成了10种4-色满酮Mannich碱类化合物,其组成和结构经熔点、红外光谱和核磁共振氢谱确证,其中6个(5d~5g,5i~5j)目标化合物均未见文献报道。采用Born's比浊法对目标化合物进行了抗血小板聚集活性的体外筛选,实验结果表明,目标化合物对二磷酸腺苷(ADP)诱导的家兔血小板聚集均具有显著的体外抑制活性。 相似文献
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α,β-不饱和环戊酮的Mannich碱和α,β-不饱和环己酮的Mannich碱具有显著的抗炎活性,为了寻求新的具有抗炎活性的环酮类化合物,设计了3,4-二氢-4-(1-哌啶甲基)-5H-1-苯并氧杂-5-酮盐酸盐作为目标化合物。以苯酚、γ-丁内酯、甲醛和哌啶等原料合成了目标化合物,并利用熔点、红外光谱、核磁共振氢谱等手段确定了其结构。采用二甲苯致小鼠耳肿胀法,测定了该化合物的抗炎活性,实验结果表明在200mg/kg剂量下该化合物对二甲苯所致小鼠耳肿胀的抑制率为54.5%。采用Born's比浊法测定了该化合物的抗血小板聚集活性,实验结果表明该化合物的抗血小板聚集活性比噻氯匹啶强约23倍。 相似文献
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《Inorganic chemistry communications》2007,10(4):410-414
Two new lead-carboxylate complexes based on nicotinic acid N-oxide ligand, [Pb(NNO)(FA)0.5] (1) (HNNO = nicotinic acid N-oxide, FA = fumaric acid) and [Pb2(NNO)(BTC)] (2) (H3BTC = 1,3,5-benzenetricarboxylic acid) were hydrothermally synthesized and characterized by the elemental analyses, IR spectra and single crystal X-ray diffraction. Significant phosphorescent properties of two compounds were observed at room temperature. 相似文献
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Hung-Cheng Shih Ching-Yuh Chern Ping-Chung Kuo You-Cheng Wu Yu-Yi Chan Yu-Ren Liao Che-Ming Teng Tian-Shung Wu 《International journal of molecular sciences》2014,15(3):3926-3951
The present study was aimed at discovering novel biologically active compounds based on the skeletons of gingerol and shogaol, the pungent principles from the rhizomes of Zingiber officinale. Therefore, eight groups of analogues were synthesized and examined for their inhibitory activities of platelet aggregation induced by arachidonic acid, collagen, platelet activating factor, and thrombin. Among the tested compounds, [6]-paradol (5b) exhibited the most significant anti-platelet aggregation activity. It was the most potent candidate, which could be used in further investigation to explore new drug leads. 相似文献
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Metal-free (H2Pc) and metallophthalocyanines (MPc; M: Co, Zn) with four n-pentyl ester of thioglycolic acid groups have been synthesized by the esterification of the corresponding carboxylic acid derivatives with n-pentanol. The novel phthalocyanine compounds were characterized by elemental analyses, mass, FT-IR and UV-Vis spectral data. The aggregation investigations carried out in different concentrations and solvents indicate that ester substituted metal-free and metallo-phthalocyanine compounds have not shown any aggregation behavior in the concentration range of about 10−5 M. Electrochemical and in-situ spectroelectrochemical measurements give common MPc based redox behaviors which supported the proposed structure of the complexes. While CoPc gives both metal-based and ring-based redox processes, H2Pc and ZnPc give only ring-based electron transfer processes. In-situ electrocolorimetric method was applied to investigate the color of the electro-generated anionic and cationic forms of the complexes. 相似文献
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以环氧乙烷为起始原料,经与甲胺水溶液进行加成反应,再与环氧氯丙烷进行烷基化反应后同时水解反应,而后与茶碱缩合反应,再与5-氧代-1-溴己烷烷基化,最后与烟酸成盐共五步反应合成得到创新药烟酸己替胺碱,并进行质谱和核磁共振氢谱的结构表征,该方法原料易得,反应条件温和,危险性小,后处理简单,易操作、产率高及易工业化的特点。 相似文献
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Baldwyn Torto Peter G. N. Njagi Ahmed Hassanali Habert Amiani 《Journal of chemical ecology》1996,22(12):2273-2281
Hexanal, octanal, nonanal, decanal, hexanoic acid, octanoic acid, nonanoic acid, and decanoic acid were identified in the volatile emissions from fifth instars ofSchistocerca gregaria by coupled gas chromatography-electroantennography (GC-EAD) detection and coupled GC-mass spectrometry (MS). In laboratory assays, synthetic blends of the eight compounds, with acids and aldehydes tested separately, evoked strong aggregation responses from fifth instars, similar to responses evoked by a crude volatile extract of the nymphs. A nymphal fecal volatile phenolic blend of guaiacol and phenol, which we have previously shown to evoke an aggregative response from different stages of the insect, significantly synergized the activity of the blend of eight compounds, suggesting mutually augmentative roles for nymphal and fecal volatiles in evoking aggregation. These results indicate that the aggregation behavior of gregarious second to fifth instars is modulated by three sets of pheromonal compounds: aldehydes and acids emitted by the nymphs themselves and phenols associated with their feces. 相似文献