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  • 标题:Green ultrasound-assisted three-component click synthesis of novel 1H-1,2,3-triazole carrying benzothiazoles and fl uorinated- -1,2,4-triazole conjugates and their antimicrobial evaluation
  • 本地全文:下载
  • 作者:NADJET REZKI ; NADJET REZKI ; MOHAMED REDA AOUAD
  • 期刊名称:Acta Pharmaceutica
  • 电子版ISSN:1846-9558
  • 出版年度:2017
  • 卷号:67
  • 期号:3
  • 页码:309-324
  • DOI:10.1515/acph-2017-0024
  • 语种:English
  • 出版社:Sciendo
  • 摘要:The present study describes an effi cient and ecofriendly,ultrasound,one- pot click cycloaddition approach for the construction of a novel series of 1,4-disubstituted-1,2,3- triazoles tethered with fl uorinated 1,2,4-triazole-benzothiazole molecular conjugates.It involved three- component condensation of the appropriate bromoacetamide benzothiazole,sodium azide and 4-alkyl/aryl-5-(2- fluorophenyl)-3-(prop-2-ynylthio)-1,2,4-triazoles 4a-e through a Cu(I)-catalyzed 1,3-dipolar cycloaddition reaction.This approach involves in situ generation of azidoacetamide benzothiazole,followed by condensation with terminal alkynes in the presence of CuSO4/Na-ascorbate in aqueous DMSO under both conventional and ultrasound conditions.Some of the designed 1,2,3-triazole conjugates 6a-o were recognized for their antimicrobial activity against some bacterial and fungal pathogenic strains.
  • 关键词:benzothiazoles;1;2;3-triazoles;1;2;4-triazoles;click synthesis;antimicrobial
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