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A facile greener synthesis, antimicrobial evaluation and molecular modelling of new 4-aryl-2-(3-(2-(trifluoromethyl)phenyl)-1,8-naphthyridin-2-yl)phthalazin-1(2H)-one derivatives

  • Boda Sakram
  • Dharavath Ravi
  • Mutyala Raghupathi
  • Boda Sathish Kumar
  • P. V. Anantha Lakshmi
Article
  • 16 Downloads

Abstract

The synthesis of 4-aryl-2-(3-(2-(trifluoromethyl)phenyl)-1,8-naphthyridin-2-yl)phthalazin-1(2H)-ones was performed by cyclization of 2-hydrazinyl-3-(2-(trifluoromethyl)phenyl)-1,8-naphthyridine with 2-aroylbenzoic acids in ethanol containing a catalytic amount of concentrated sulfuric acid under solid state conditions. All these synthesized compounds (8ah) were screened for their in vitro antibacterial activity against gram-positive bacteria such as (Staphylococcus aureus) and gram-negative bacteria (Escherichia coli) and also evaluated for their antifungal activity against Aspergillus Niger and Helmenthosphorium oryzae fungal strains. Some of the products demonstrate good antibacterial activity and moderate antifungal activity. In predominantly, 8b, 8d, 8g, and 8h compounds showed good to excellent antibacterial and antifungal activities. The antimicrobial activity of the compound 8 was further investigated with the help of in LibDock score docking study to predict the active sites.

Graphical abstract

Keywords

Greener chemistry 1,8-Naphthyridines Biological activity Molecular docking 

Notes

Acknowledgements

The authors are thankful to the Head, Department of Chemistry, Osmania University, for providing laboratory facilities and constant encouragement, and are also thankful to the Directors, IICT, CFRD-OU-Hyderabad, for providing spectral and analytical data of the synthesized compounds. One of the authors (Dharavath Ravi) is thankful to the UGC-SRF New-Delhi, India, for the financial support.

Supplementary material

11164_2018_3711_MOESM1_ESM.docx (3.3 mb)
Supplementary material 1 (DOCX 3353 kb)

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Copyright information

© Springer Nature B.V. 2019

Authors and Affiliations

  1. 1.Department of ChemistryOsmania UniversityTarnaka, HyderabadIndia
  2. 2.Department of ChemistryCSIR-Indian Institute of Chemical TechnologyTarnakaIndia

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