Synthesis and Antibacterial Activities of Sulfonamides Derivatives Bearing 1, 2, 3-Triazole Moiety
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the Natural Science Foundation of Guangxi Zhuang Autonomous Region (2015GXNSFAA139035, 2016GXNSFAA380323); the Major Program of the Natural Science Foundation of Guangxi Zhuang Autonomous Region (2016GXNSFEA380001); Undergraduate Innovation and Entrepreneurship Training Program(201510601020); the Key Project of Scientific Research and Technology Development of Guilin.

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    Abstract:

    The Intermediate 2-chloro-N-(4-sulfamoylphenyl)acetamide(II) was obtained by the reaction of sulfanilamide and chloroacetyl chloride. Ten 1, 2, 3-triazolyl sulfonamides were prepared using a known one-pot procedure starting from (II), sodium azide and terminal alkynes. The target compounds were characterized by FTIR, 1H NMR, 13C NMR and ESI-MS. The minimal inhibitory concentrations (MIC) of target compounds against S.aureus and E.coli were determined with double broth dilution method. The results showed that all the tested compounds exhibited a certain antibacterial activities. In particular, 2-(4-(3-fluorophenyl)-1H-1, 2, 3-triazol-1- yl)-N-(4- sulfamoylphenyl)acetamide (IIIh) possessed similar activity against E.coli compared with the positive control drug (ciprofloxacin 0.25 μg/mL).

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History
  • Received:March 24,2018
  • Revised:July 23,2018
  • Adopted:July 24,2018
  • Online: November 08,2018
  • Published:
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