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为探索α,β-不饱和酮结构的抑癌活性,设计合成了7个2-取代亚甲基环戊酮(Ⅰa~g),5个2-烷基环戊烯酮(Ⅱb~f)和4个2-烷氧基环戊烯酮(Ⅲa~d)等共16个含有α,β-不饱和酮结构的化合物,其中2-苄氧基环戊烯酮(Ⅲc)和环己氧基环戊烯酮(Ⅲd)为未见文献报道的化合物.体外抑癌筛选结果证实,某些化合物具有一定的抑癌活性  相似文献   

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A series of tetrachlorophthalic acid derivatives were obtained by acylating primary amines with tetrachlorophthalic anhydride under mild conditions. Antibacterial activity of the synthesized compounds with respect to Escherichia coli and Staphylococcus aureus was studied in vitro by the serial dilution technique. The most pronounced antimicrobial effect in the series of compounds tested was observed for 2-hydroxyphenylamide of tetrachlorophthalic acid; 4-antipyrylamide of tetrachlorophthalic acid showed a significant antiinflammatory activity. __________ Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 39, No. 8, pp. 16 – 18, August, 2005.  相似文献   

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A series of N-l,N′-(n + 2)-bis[3-cyano(ethoxycarbonyl)-4,5-dimethylthiophen-2-yl]alkanediamides have been synthesized by acylating 4,5-dimethyl-2-amino-3-cyano(ethoxycarbonyl)thiophenes with the corresponding dicarboxylic acid dichloroanhydrides. The results of biological tests show that the obtained bisamides possess antiinflammatory and analgesic (non-narcotic) activity. __________ Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 39, No. 6, pp. 26 – 27, June, 2005.  相似文献   

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Pharmaceutical Chemistry Journal - Aseries 6-phenyl-2-(substituted methyl)-dihydropyridazinone derivatives (3a–3f) were synthesized using the interaction of 6-phenylpyridazinone with cyclic...  相似文献   

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通过取代溴苄与1-(2,4-二取代苯基)-2-(1H-吲哚和苯并咪唑-1-基)乙醇反应,合成了一系列1-{2-「(取代苯基)甲基」-2-(取代苯基)乙基-1-吲哚和苯并咪唑类新化合物,并用二倍体稀释法对化合物进行了体外抗真菌试验。  相似文献   

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酚取代双膦酸酯Schiff碱的合成及抗癌活性研究   总被引:1,自引:0,他引:1  
设计合成了11个含有Schiff碱双键的酚取代双膦酸酯类化合物。对小鼠白血病细胞P388、人肺腺癌细胞A-549的体抗癌活性实验表明:目标分子中酚羟基的位置对化合物的活性有着重要影响,当酚羟基位于Schiff碱双键的邻位时,其活性高于其他化合物。  相似文献   

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New coordination compounds of copper(II) with thiosemicarbazones of 5-chloro-, 5-bromo-, 5-nitro-, 5-methyl-, 3,5-dichloro-, and 3,5-dibromo-substituted salicylaldehyde have been synthesized and tested with respect to eight strains of staphyloccoccus, streptococcus, and colon bacillus. These compounds exhibit high antimicrobial activity. The composition and structure of the synthesized complexes have been studied by means of elemental analysis and by magnetochemical, IR, and thermogravimetric techniques. The antimicrobial activity of the obtained coordination compounds depends both on the nature of substituents in the benzene ring of salicylaldehyde and on the nature of acid ligands. The maximum antimicrobial activity was observed for copper(II) complexes with thiosemicarbazone of 3,5-dibromsalicyladehyde. __________ Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 39, No. 6, pp. 30 – 32, June, 2005.  相似文献   

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设计合成了14个4-取代氨基-6-苯嘧啶类化合物,小鼠MES抗惊实验结果表明:所合成的化合物及中间体都有不同程度的抗惊活性。其中(Ⅱ9)和(Ⅱ13)抗惊活性最强,甚至超过对照品苯妥英钠,初步推测,4位氨基氮原子上取代基的空间结构对抗惊活性有重要影响。  相似文献   

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