Novel 5-Nitro Isatin derivatives as DNA Gyrase inhibitors: synthesis, anti-microbial evaluation, molecular docking, ADMET predictions and QSAR studies

Authors

  • walaa S El-serwy National Research Centre
  • Neama A Mohamed National Research Centre
  • Emad M. M Kassem National Research Centre
  • Eman S. Nossier Al-Azhar University
  • Al Shimaa G. Shalaby National Research Centre

Keywords:

Antibacterial, Antifungal, Antimicrobial, DNA_gyrase B, Heterocycles, Gyrase Inhibitors

Abstract

Novel series of 5-nitroindoline-2-ones was synthesized starting from 5-nitroindoline-2,3-dione 2 and 2-(5-nitro-2-oxoindolin-3-ylidene)hydrazine-1 carbothioamide 3. Compounds were evaluated for their antimicrobial activities. The data showed that compounds 2 and 6b have excellent antimicrobial activities against the two tested strains of G+ve bacteria Staphylococcus aureus and Streptococcus and E. coli when compared with the standards. Furthermore, in-vitro enzyme assay and molecular docking studies were performed for the compounds 2 and 6b against E. coli DNA gyrase B. Prediction of ADMET properties and QSAR study of compounds was carried out respectively.

Gyrase inhibitor isatin heterocycles

Published

2020-07-31

How to Cite

El-serwy, walaa S. ., Mohamed, N. A. ., Kassem, E. M. M. ., Nossier, E. S. ., & Shalaby, A. S. G. . (2020). Novel 5-Nitro Isatin derivatives as DNA Gyrase inhibitors: synthesis, anti-microbial evaluation, molecular docking, ADMET predictions and QSAR studies. Chemical Biology Letters, 7(4), 197-206. Retrieved from http://thesciencein.org/journal/index.php/cbl/article/view/51

Issue

Section

Research Articles