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  • 标题:Utility of Lauroyl Isothiocyanate as a Scaffold in the Synthesis of Some Novel Pyrimidine Derivatives and Their Antimicrobial Assessment
  • 作者:Heba Kamal Abd El-Mawgoud ; Magdy Mohamed Hemdan
  • 期刊名称:Chemical and Pharmaceutical Bulletin
  • 印刷版ISSN:0009-2363
  • 电子版ISSN:1347-5223
  • 出版年度:2018
  • 卷号:66
  • 期号:11
  • 页码:1072-1077
  • DOI:10.1248/cpb.c18-00595
  • 语种:English
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:The reaction of lauroyl isothiocyanate 1 with enaminonitrile derivative 2 furnished N -(6-cyano-3, 4-diphenylthieno[2,3- c ]pyridazin-5-yl-carbamothioyl)dodecanamide 3 , which was used as precursor for the synthesis of novel heterocyclic systems. Polyfunctional pyrimidine and fused pyrimidine derivatives were obtained by the cyclization of compound 3 under different basic conditions as well as its reactions with thiourea, o -aminothiophenol, hydrazine hydrate, phenyl hydrazine, ethyl phenyl acetate or ethyl benzoyl acetate. The structures of the new compounds were confirmed by microanalytical and spectral properties. The synthesised compounds were tested in-vitro for their antimicrobial activity and showed congruent results against most of the tested microorganisms compared to the standard drugs Gentamycin and Ketoconazol.
  • 关键词:lauroyl isothiocyanate;enaminonitrile;pyrimidine;fused pyrimidine;antimicrobial screening
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