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新型胆酸不对称双缩二氨基硫脲类衍生物的合成及其抗菌活性 被引量：2

Synthesis and Antibacterial Activities of Novel Cholic Acid Asymmetric Bis Thiosemicarbazone Derivatives
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摘要 在微波辐射条件下,甾酮与取代单缩二氨基硫脲经缩合反应合成了12个新型的胆酸不对称双缩二氨基硫脲衍生物(3a^3l),其结构经1H NMR,IR,ESI-MS和元素分析表征。初步抗菌活性测定结果表明:部分化合物对枯草芽孢杆菌、金黄色葡萄球菌、大肠杆菌及绿脓杆菌有一定的抗菌活性,其中,1-(2-羟基苯苄叉基)-5-[3-(3,7-二氧代-24-胆烷酸甲酯)亚甲基]二氨基硫脲(3f)对大肠杆菌的抑菌活性(IC507.40)与阿莫西林(IC507.30)相当。 Twelve novel cholic acid asymmetric bis thiosemicarbazone derivatives（3a-31） were syn- thesized by condensation of steroidal ketones with substituted thiosemicarbazides under microwave ir- radiation. The structures were characterized by 1H NMR, IR, ESI-MS and elemental analysis. Pre- liminary antibacterial activities tests indicated）that some compounds exhibited certain inhibitory activi- ties against Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomanus aeroginosa. 1- （2-Hydroxybenzylidene） -5- [ 3- （7,12-dioxo-24-cholanate） methylene ] thiocarbohydrazide （3f） showed inhibitory activities（ IC50 7.40） as same as Amoxicillin（ IC50 7.30） against Escherichia coli.
作者 张丽娜 赵志刚 谭炯 李晖
机构地区 西南民族大学化学与环境保护工程学院
出处 《合成化学》 CAS CSCD 2015年第8期677-682,共6页 Chinese Journal of Synthetic Chemistry
基金 四川省科技支撑计划项目(2012SZ0160) 西南民族大学研究生创新型科研项目(CX2014SZ43)
关键词 胆酸 缩氨基硫脲 微波合成 抗菌活性 cholic acid thiosemicarbazone microwave synthesis antibacterial activity
分类号 O621.3 [理学—有机化学] O629.2 [理学—有机化学]
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参考文献28

  • 1胡云霞,李琬聪,周婷婷,郭占勇.1,2,3-三氮唑桥连水杨醛类席夫碱菊糖衍生物的合成及抑菌活性研究[J].化学与生物工程,2014,31(8):27-30. 被引量：4
  • 2Abdel M A A, Mohamed E Z, Suliman A A. Synthe- sis, spectral characterization, molecular modeling and antimicrobial studies of tridentate azo-dye Sehiff base metal complexes [ J ]. J Mole Struct ,2015,1084:36 - 45.
  • 3仇晓阳.二核双席夫碱铜(Ⅱ)配合物的合成、晶体结构及抗菌活性研究(英文)[J].无机化学学报,2014,30(7):1667-1672. 被引量：8
  • 4胡庆红,袁泽利,吴庆,张铭钦,朱必学.二氨基硫脲双核席夫碱和其配合物的合成与抗菌活性[J].应用化学,2009,26(5):534-537. 被引量：13
  • 5Gustavo E C, Michael R H, Wara M A, et al. Initial evaluation of the antitumour activity of KGP94, a func-tionalized benzophenone thiosemicarbazone inhibitor of cathepsin L[ J ]. Eur J Med Chem,2012,58:568 - 572.
  • 6Ana I M, Ines L, Pilar S. Palladium( II ) and plati- num ( II ) bis (thiosemicarbazone) complexes of the 2, 6-diacetylpyridine series with high cytotoxic activity in cisplatin resistant A2780cisR tumor ceils and reduced toxicity [ J ]. J Inorg Biochem,2013,125 : 26 - 31.
  • 7Floyd A B, Jeffrey T, Michael S J, et al. Synthesis and characterization of mixed-ligand diimine-piperonal thiosemicarbazone complexes of ruthenium ( II ) : Bio- physical investigations and biological evaluation as an- tieancer and antibacterial agents [ J ]. J Mole Struct, 2011,992:39 -47.
  • 8Duraippandi P, Ashoka G S. Dinuclear zinc bis (thio- semicarbazone) complexes : Synthesis, in vitro antican- cer activity, cellular uptake and DNA interaction stud- ys[ J]. Inorg Chim Acta,2013,405 : 152 - 161.
  • 9Field H J, Reading M J. The inhibition of bovine her- pesvirus-1 by methyl 2-pyridyl ketone thiosemicarba- zone and its effects on bovine cell [ J ]. Antiviral Res, 1987,7:245 - 256.
  • 10Andreas J K. Broad-spectrum antiviral activity inclu- ding human immunodeficiency and hepatitis C viruses mediated by a novel retinoid thiosemicarbazone deriv- atives[J]. Eur J Med Chem,2011,46:1656 - 1664.

二级参考文献175

共引文献59

同被引文献21

  • 1SHELKE S H, MHASKE P C, KASAM S K, et al. Synthesis and phar- macological evaluation of a novel series of 2-( ( 2-Aryl thiazol-4-yl ) methyl) -5-( alkyl/alkylnitrile thio ) -1,3,4-oxadiazole derivatives as possible antifungal agents [ J ]. Journal of Heterocyclic Chemistry, 2014, 51(6) :1893-1897.
  • 2AZIZI N, GHOLIBEGHLO E, MANOCHERI Z, et al. Green procedure for the synthesis of bis(indolyl) methanes in water[ J ]. Scientia Iranica C,2012,19(3) :574-578.
  • 3HENRIK J ,TANJA B J, DAVID E G, et al. 3-Substituted 2-phenyl-in- doles:privileged structures for medicinal chemistry [ J ]. RSC Advances, 2013,3(3) :945-960.
  • 4HASSAM M, BASSON A E, LIOTrA D C, et al. Novel eyelopropyl-In- dole derivatives as HIV non-nucleoside reverse transcriptase inhibitors [ J]. ACS Medicinal Chemistry Letters ,2012,3 (6) :470-475.
  • 5EL-NAGA R N,AHMED H I,ABD AL HALEEM E N. Effects of in- dole-3-carbinol on clonidine-indueed neurotoxicity in rats: Impact on oxidative stress, inflammation, apoptosis and monoamine levels [ J ]. Neurotoxicology,2014,44( 1 ) :48-57.
  • 6SONG Y L,WU F,ZHANG C C, et al. Ionic liquid catalyzed synthesis of 2- ( indole-3-yl ) -thiochmman-4--ones and their novel antifungal activi- ties[J]. Bioorganic & Medicinal Chemistry Letters,2015,25 (2) :259- 261.
  • 7KAUSHIK N K, KAUSHIK N, ATI'RI P, et al. Biomedical Importance of Indoles [ J ]. Molecules,2013,18 ( 6 ) :6620-6662.
  • 8LEE W I, JUNG J W, SIM J, et al. Microwave-assisted synthesis of 3- substituted indoles viaintramolecular arencealkene coupling of o-iodoa- nilino enamines[J]. Tetrahedron,2013,69(35) :7211-7219.
  • 9SRINIVAS V, KOKETSU M. Synthesis of indole-2-, 3-, or 5-substituted propargylamines via.gold( IlI)-catalyzed three component reaction of al- dehyde, alkyne, and amine in aqueous medium [ J ]. Tetrahedron, 2013, 69( 37 ) :8025-8033.
  • 10ASIRI A M, KHAN S A. Palladium(11) complexes of NS donor ligandsderived from steroidal thiosemicarbazones as antibacterial agents [ J ]. Molecules,2010,15 (7) :4784-4791.

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合成化学
2015年 第8期

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