• 文献标题:   Ultrasound-Assisted Synthesis of Nitrogen and Oxygen Containing Heterocycles Using Fluorinated Graphene Oxide as Catalyst: Evaluation of Their Anthelmintic Activities
  • 文献类型:   Article
  • 作  者:   DUTTA A, CHHETRI B, NONGRUM R, KHARMAWLONG GK, YADAV AK, NONGKHLAW R
  • 作者关键词:   anthelmintic activitie, fluorinated graphene oxide heterocylce, molecular docking, spirooxindole
  • 出版物名称:   CHEMISTRYSELECT
  • ISSN:   2365-6549
  • 通讯作者地址:   North Eastern Hill Univ
  • 被引频次:   0
  • DOI:   10.1002/slct.202001442
  • 出版年:   2020

▎ 摘  要

Spirooxindole derivatives have been efficiently synthesizedviaa three-component reaction consisting of isatin, malononitrile/ pyrazole and various 1,3-diketones using Fluorinated Graphene Oxide (FGO) as a green and metal free carbocatalyst, under sonication. The main advantages of this synthetic approach lie in its operational simplicity, easy catalyst recovery and recyclability, high yields and short reaction times. The prepared catalyst was characterized by various analytical techniquesviz.,UV-Vis,FT-IRSpectroscopy,TGA,TEM,FE-SEMandEDX. The in vitro anthelmintic screening of synthesized compounds against a cestode,Raillietinasp. and a nematode parasite,Syphacia obvelataat 200 mu g/mL and 800 mu g/mL were also carried out which revealed a profound activity, with much reduced morality time of parasite. The SEM study indicated structure alterations in treated parasite, further validating the in vitro anthelmintic property. In addition, molecular docking studies were carried out against beta-tubulin protein to determine binding affinity of the synthesized compounds. All test compound followed the "Lipinski Rule of Five" and in silico pharmacokinetic investigation showed inhibitory activity against CYP enzyme and P-glycoprotein which may further improve the bio efficacy of compounds.