欢迎登录材料期刊网

材料期刊网

高级检索

在微波辅助下,l,3-二甲基-5-醛基巴比妥酸与芳氧基/芳胺基乙酰肼及含氮杂环乙酰肼缩合制备新型酰腙化合物,并对其抑菌活性进行评价的研究.新化合物的结构经过元素分析、红外光谱、核磁共振谱、质谱和X射线单晶衍射等技术手段确认.体外的抑菌活性实验显示,部分目标化合物呈现出优于环丙沙星的抑菌活性.经过构效关系分析表明,当芳基为含氮杂环时,所形成的化合物抗菌活性与芳基为苯环时相比明显较强,抑菌活性最强的酰腙化合物2t对金黄色葡萄球菌的最小抑菌浓度(MIC)值为0.8 g/L,对大肠杆菌的最小抑菌浓度(MIC)值为1.6 g/L.

参考文献

[1] A. Habibi;Z. Tarameshloo.A New and Convenient Method for Synthesis of Barbituric Acid Derivatives[J].Journal of the Iranian Chemical Society,20111(1):287-291.
[2] Jursic BS.;Stevens ED..Transition metal free reductive dimerization of nitrogen containing barbituric acid benzylidenes[J].Journal of Heterocyclic Chemistry: The International Journal of Heterocyclic Chemistry,20034(4):701-706.
[3] Nevagi, Reshma J.;Dighe, Santosh N.;Dighe, Satish N.;Chaskar, Pratip K.;Srinivasan, Kumar V.;Jain, Kishor S..Use of Ionic Liquids as Neoteric Solvents in the Synthesis of Fused Heterocycles[J].Archiv der Pharmazie,20148(8):540-551.
[4] Alizadeh, Abdolhamid;Khodaei, Mohammad Mehdi;Fakhari, Mitra;Abdi, Gisya;Ghouzivand, Sohrab.Chemo and regioselective serendipitous electrochemically initiated spirocyclization of caffeic acid esters with barbituric acid derivatives[J].Electrochimica Acta,2015:533-540.
[5] Cunha, TM;Roman-Campos, D;Lotufo, CM;Duarte, HL;Souza, GR;Verri, WA;Funez, MI;Dias, QM;Schivo, IR;Domingues, AC;Sachs, D;Chiavegatto, S;Teixeira, MM;Hothersall, JS;Cruz, JS;Cunha, FQ;Ferreira, SH.Morphine peripheral analgesia depends on activation of the PI3K gamma/AKT/nNOS/NO/K-ATP signaling pathway[J].Proceedings of the National Academy of Sciences of the United States of America,20109(9):4442-4447.
[6] Moamen S. Refat;Abdel Majid A. Adam.Structural, thermal, kinetic and pharmacology in vitro studies of H-bonded complexes formed between the sedative-hypnotic drug 5,5-diethylbarbituratic acid with various acceptors: Liquid and solid characterization[J].Journal of Molecular Liquids,2014:142-152.
[7] Neumann,D.M.;Cammarata,A.;Backes,G.;Palmer,G.E.;Jursic,B.S..Synthesis and antifungal activity of substituted 2,4,6-pyrimidinetrione carbaldehyde hydrazones[J].Bioorganic and medicinal chemistry,20142(2):813-826.
[8] Teimouri, M.B.;Akbari-Moghaddam, P.;Motaghinezhad, M..Urotropine-bromine promoted synthesis of functionalized oxaspirotricyclic furopyrimidines via a domino Knoevenagel condensation/Michael addition/α-bromination/Williamson cycloetherification sequence in water[J].Tetrahedron,201333(33):6804-6809.
[9] 夏庆春;何其庄;沈智慧;许东芳.芳酰肼的制备及表征[J].上海师范大学学报(自然科学版),2009(5):506-510.
[10] Husain A;Ahmad A;Alam MM.Fenbufen based 3-(5-(substituted aryl)-1,3,4-oxadiazol-2-yl)-1-(biphenyl-4-yl)propan-1-ones as safer antiinflammatory and analgesic agents.[J].European Journal of Medicinal Chemistry,20099(9):3798-3804.
[11] Siddiqui N;Alam MS;Ahsan W.Synthesis, anticonvulsant and toxicity evaluation of 2-(1H-indol-3-yl)acetyl-N-(substituted phenyl)hydrazine carbothioamides and their related heterocyclic derivatives.[J].Acta pharmaceutica: a quarterly journal of Croatian Pharmaceutical Society and Slovenian Pharmaceutical Society, dealing with all branches of pharmacy and allied sciences,20084(4):445-454.
[12] Jadav, Surender Singh;Kaptein, Suzanne;Timiri, Ajaykumar;De Burghgraeve, Tine;Badavath, Vishnu Nayak;Ganesan, Ramesh;Sinha, Barij Nayan;Neyts, Johan;Leyssen, Pieter;Jayaprakash, Venkatesan.Design, synthesis, optimization and antiviral activity of a class of hybrid dengue virus E protein inhibitors[J].Bioorganic and Medicinal Chemistry Letters,20158(8):1747-1752.
[13] Jitender M. Khurana;Kanika Vij.Nickel Nanoparticles Catalyzed Knoevenagel Condensation of Aromatic Aldehydes with Barbituric Acids and 2-Thiobarbituric Acids[J].Catalysis Letters,20101/2(1/2):104-110.
[14] Sathisha KR;Khanum SA;Chandra JN;Ayisha F;Balaji S;Marathe GK;Gopal S;Rangappa KS.Synthesis and xanthine oxidase inhibitory activity of 7-methyl-2-(phenoxymethyl)-5H-(1,3,4)thiadiazolo(3,2-a)pyrimidin-5-one derivatives.[J].Bioorganic and medicinal chemistry,20111(1):211-220.
[15] More,U.A.;Joshi,S.D.;Aminabhavi,T.M.;Gadad,A.K.;Nadagouda,M.N.;Kulkarni,V.H..Design, synthesis, molecular docking and 3D-QSAR studies of potent inhibitors of enoyl-acyl carrier protein reductase as potential antimycobacterial agents[J].European Journal of Medicinal Chemistry: Chimie Therapeutique,2014:199-218.
上一张 下一张
上一张 下一张
计量
  • 下载量()
  • 访问量()
文章评分
  • 您的评分:
  • 1
    0%
  • 2
    0%
  • 3
    0%
  • 4
    0%
  • 5
    0%