4.7 Article

Synthesis, crystal structure and antimicrobial potential of some fluorinated chalcone-1,2,3-triazole conjugates

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 155, Issue -, Pages 263-274

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2018.05.055

Keywords

Fluoronated compounds; Chalcones; 1,2,3-Triazoles; Antimicrobial activity; Docking studies

Funding

  1. Haryana State Council for Science and Technology (HSCST)
  2. DST, New Delhi [SR/PURSE 2/40(G)]

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A simple and green synthesis of some fluorinated chalcone-triazole hybrids from propargylated chalcones and organic azides catalyzed by cellulose supported copper nanoparticles click reaction is reported. All the synthesized compounds were well characterized by various analytical and spectroscopic methods. The X-rays crystallographic study of compounds 6k revealed the self assembling properties. The antimicrobial screening results of all the synthesized compounds revealed that most of the triazole hybrids exhibited significant efficacy against tested bacterial and fungal strains. The activity results showed the synergistic effect of biological activity when two pharmacophoric units, i.e. chalcone and 1,2,3-triazole are conjugated. Further, docking simulation of the most active compounds 6p into Escherichia coli topoisomerase II DNA Gyrase B was also carried out. (C) 2018 Elsevier Masson SAS. All rights reserved.

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