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

被引:96
|
作者
Yadav, Pinki [1 ]
Lal, Kashmiri [1 ]
Kumar, Lokesh [1 ]
Kumar, Ashwani [2 ]
Kumar, Anil [3 ]
Paul, Avijit K. [4 ]
Kumar, Rajnish [5 ]
机构
[1] Guru Jambheshwar Univ Sci & Technol, Dept Chem, Hisar 125001, Haryana, India
[2] Guru Jambheshwar Univ Sci & Technol, Dept Pharmaceut Sci, Hisar 125001, Haryana, India
[3] Guru Jambheshwar Univ Sci & Technol, Dept Bio & Nanotechnol, Hisar 125001, Haryana, India
[4] Natl Inst Technol, Dept Chem, Kurukshetra 136119, Haryana, India
[5] Karolinska Inst, Div Neurogeriatr, Ctr Alzheimer Res, Dept Neurobiol Care Sci & Soc, Huddinge, Sweden
关键词
Fluoronated compounds; Chalcones; 1,2,3-Triazoles; Antimicrobial activity; Docking studies; ONE-POT SYNTHESIS; BIOLOGICAL EVALUATION; 1,4-DISUBSTITUTED 1,2,3-TRIAZOLES; MEDICINAL CHEMISTRY; CLICK CHEMISTRY; BETA-LACTAM; CHALCONES; AGENTS; HYBRIDS; DESIGN;
D O I
10.1016/j.ejmech.2018.05.055
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:263 / 274
页数:12
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