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2-氨基-4H-咪唑啉-4-酮衍生物的快速平行合成法 总被引:3,自引:0,他引:3
咪唑啉酮衍生物是一类具有良好生物活性和药理活性的杂环化合物 [1,2 ] ,尤其是一些 2 -氨基咪唑啉酮表现出良好的杀菌、抗炎及抗癌活性 [3 ,4 ] .从自然界如一些海洋生物中可分离得到含 2 -氨基咪唑啉酮结构的生物碱 [5,6] .最近 ,组合化学方法广泛地应用于有机合成 ,它包括固相合成法和液相合成法[7~ 9] .我们曾应用氮杂 Wittig反应制得 2 -氨基取代咪唑啉酮衍生物 ,部分化合物表现出一定的抑菌活性 [10 ,11] .本文进一步报道应用液相平行反应法快速合成 2 -氨基 - 4H-咪唑啉 - 4-酮衍生物 (4) .该方法应用烯基膦亚胺 1与苯基异氰酸酯的… 相似文献
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《有机化学》2020,(5)
以朝格尔碱衍生物(5,12-二甲基-3,10-二苯基-双-1H-吡唑[b,f][4,5]-1,5-二氮杂双环[3.3.1]-2,6-辛二烯,1)为催化剂,以取代的α-溴代苯乙酮、芳香醛、丙二腈和硫脲为原料四组分一锅法合成了一系列噻唑并[3,2-a]嘧啶衍生物.通过1H NMR和化学实验探讨了该反应的机理.体外药理活性实验结果表明,多个产物对人肝癌细胞(Hep G2)、人非小细胞肺癌细胞(247)和人非小细胞肺癌细胞(A549)中的一个或多个细胞株具有较高抑制活性,七个产物对耐甲氧西林金黄色葡萄球菌具有抑菌活性.这些结果表明该类化合物在新药开发中具有巨大潜力. 相似文献
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6-(4-取代苯基)-5-甲基-4,5二氢-3(2H)哒嗪酮化合物的合成及其抑制血小板聚集作用 总被引:3,自引:0,他引:3
血小板聚集在血栓形成中起着先导而关键的作用,而严重威胁人类生命健康的心脑血管疾病多数与血栓形成和血栓栓塞有着密切的联系[1]。二氢哒嗪酮类化合物对抑制血小板聚集有较强的药理活性,对二磷酸腺苷(ADP)、花生四烯酸(AA)、血小板活化因子(PAF)和胶原(Collagen)引起的血小板聚集均有抑制作用。深入研究二氢哒嗪酮类化合物的构效关系,以期寻找活性更强的抗血小板聚集药物,是开发新型心脑血管系统疾病药物的重要研究方向之一。本文设计合成了6-(4-取代苯基)-5-甲基-4,5二氢-3(2H)哒嗪酮类化合物[2,3,4],并进行了体外药理实验。1实验部… 相似文献
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将5-取代胺基-2-巯基-1,3,4-噻二唑引入苯并[4,5]呋喃[3,2-d]嘧啶中,设计并合成了10个新型的4-(5-N-取代-1,3,4-噻二唑-2-巯基)-苯并[4,5]呋喃[3,2-d]嘧啶类衍生物(3a~3j),其结构经1H NMR,13C NMR,IR和MS确认。用MTT法测定了3a~3j对人胃腺癌细胞体(MGC)的体外增殖活性。结果表明,3a~3j均具有不同程度的抑制MGC的活性,其中4-(5-N-2’-甲氧基苯基-1,3,4-噻二唑-2-巯基)-苯并[4,5]呋喃[3,2-d]嘧啶(3j)在10μmol·L-1的浓度下对MGC的抑制率为86.4%。 相似文献
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S-烃基-1-烃基-3-[4-(苯并咪唑-2-巯基)苯基]异硫脲的合成及其iNOS抑制活性 总被引:4,自引:0,他引:4
以2-巯基苯并咪唑(1)为原料,经缩合和还原得到2-(4-氨基苯硫基)苯并咪唑(3),再与异硫氰酸苯甲酰酯或异硫氰酸烃基酯反应得到取代硫脲(5和7),最后与卤代烃反应得到20个新的S-烃基-1-烃基-3-[4-(苯并咪唑-2-巯基)苯基]异硫脲化合物(6和8),其结构经IR,1HNMR,MS及元素分析确证.初步的药理试验表明,20个目标化合物均有不同程度的iNOS抑制活性,其中化合物6b,8d和8f的iNOS抑制活性与阳性对照药氨基胍相当. 相似文献
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N-Substituted 1,6-dihydro-3(2H)-pyridinones have been synthesised from N-substituted piperidine-3,5-diones via the methyl enol ethers. Reduction of the latter with sodium borohydride (NaBH4) is described. 相似文献
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A. L. Lapidus L. Yu. Brezhnev M. M. Vartanyan E. Yu. Vol'f T. Yu. Solov'eva B. I. Ugrak A. P. Rodin 《Russian Chemical Bulletin》1990,39(8):1667-1670
N-Substituted 3- and 4-formylpyrroles have been obtained by hydroformamination of 2,5-dimethoxy-2,5-dihydrofurans in the presence of HRh(CO)(PPh3)3.Translated from Izvestiya Akademii Nauk SSSR, Seriya Khimicheskaya, No. 8, pp. 1837–1840, August, 1990. 相似文献
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S. N. Shurov Yu. S. Andreichikov S. S. Berestova 《Chemistry of Heterocyclic Compounds》1989,25(4):441-444
N-Substituted 2-imino-5-aryl-2,3-dihydro-3-furanones react with o-phenylenediamine to form N-substituted 2-amino-3-phenacylidene-3,4-dihydroquinoxalines.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 4, pp. 528–531, April, 1989. 相似文献
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N-Substituted 3-carbamoylpyridinium salts were reduced by glyceraldehyde to give 1,4-dihydronicotinamide derivatives, which may be regarded as a model for oxidation by glyceraldehyde-3-phosphate dehydrogenase. 相似文献
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N-Substituted amides of some aliphatic and aromatic acids, respectively, have been obtained by the acylation and aroylation of 4-amino-1,2,5-trimethylpiperidine. 相似文献
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O. V. Artemova O. S. Vasil’eva E. S. Ostroglyadov M. M. Zobacheva V. M. Berestovitskaya 《Russian Journal of General Chemistry》2009,79(10):2201-2206
N-Substituted 3-methoxycarbonyl-4-phenyl-2-pyrrolidones react with 2-aryl(heteryl)-1-nitroethenes as typical CH-acids to give nucleophilic addition products. The structure of compounds obtained was studied by IR, 1H and 13C NMR spectroscopy using HOESY experiment. 相似文献
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Dostert C Wanstrath C Frank W Müller TJ 《Chemical communications (Cambridge, England)》2012,48(58):7271-7273
Quantum chemical screening reveals that 4H-dithieno[2,3-b:3',2'-e][1,4]thiazines possess the highest HOMO among four constitutional isomers, even 0.27 eV higher in energy than the well established 10H-phenothiazine. N-Substituted 4H-dithieno[2,3-b:3',2'-e][1,4]thiazines are readily accessible by twofold Pd-catalyzed amination. According to cyclic voltammetry dithienothiazines are reversibly oxidized and can be considered as new donors for functional π-systems. 相似文献
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Hai -Ming Zhang Xiu -Qin Ruan Qing -Xiang Guo You -Cheng Liu 《Research on Chemical Intermediates》1998,24(6):687-693
N-Substituted phenothiazines were oxidized by 2,2,6,6-tetramethy-4-acetyloxypiperidine oxoammonium hexachloroantimonate (TAPO)
to the corresponding radical cations in sodium dodecyl sulfate (SDS) micellar solution. The radical cations of phenothiazine
derivatives were generated and stabilized by the anionic micelle in queous solution. An electron transfer mechanism has been
proposed. 相似文献
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V. Yu. Mitskyavichyus R. S. Baltrushis Z. -I. G. Beresnevichyus 《Chemistry of Heterocyclic Compounds》1991,27(4):420-423
N-Substituted -alanines have been synthesized by treating o-aminophenol or o-benzyloxyaniline with acrylic, methacrylic, or crotonic acids. Their cyclization to 2-benzoxazolinones and dihydro-2,4(1H,3H)-pyrimidinediones has been studied.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 4, pp. 527–531, April, 1991. 相似文献
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3-(N-Substituted)amino-4-arylamino-1H-isochromenones (isocoumarins) which can be regarded as the enediamine tautomers of the Ugi four-component condensation primary adducts between 2-formylbenzoic acids, arylamines, and isocyanides undergo a facile ring cleavage with amines to give a series of phenylglycine derivatives. Thus, a synthetically useful post-condensation transformation of Ugi four-component condensation primary adducts is described for the first time. 相似文献