Synthesis, antimicrobial evaluation and docking studies of some novel quinazolinone Schiff base derivatives

Research in Pharmaceutical Sciences
Rezvan Rezaee NasabF Hassanzadeh

Abstract

The quinazolin-4(3H)-one structural motif possesses a wide spectrum of biological activities. DNA gyrase play an important role in induction of bacterial death. It has been shown that many quinazolin-4(3H)-one derivatives have antibacterial effects through inhibition of DNA gyrase. Based on this information we decided to synthesize novel quinazolinone Schiff base derivatives in order to evaluate their antibacterial effects. A series of novel quinazolinone Schiff base derivatives were designed and synthesized from benzoic acid. The potential DNA gyrase inhibitory activity of these compounds was investigated using in silico molecular docking simulation. All new synthesized derivatives were screened for their antimicrobial activities against three species of Gram-negative bacteria including Escherichia coli, Pseudomonas aeruginosa, Salmonella entritidis and three species of Gram-positive bacteria comprising of Staphylococcus aurous, Bacillus subtilis, Listeria monocitogenes as well as for antifungal activities against Candida albicans using the conventional micro dilution method. Most of the compounds have shown good antibacterial activities, especially against E. coli at 128 µg/mL concentration while no remarkable antifungal acti...Continue Reading

References

Jun 13, 2000·Protein Science : a Publication of the Protein Society·S J BlanceA Maxwell

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Citations

Nov 24, 2020·Journal of Biomolecular Structure & Dynamics·Nima SepehriIlhami Gulcin
May 22, 2021·Journal of Biomolecular Structure & Dynamics·Sartaz BegumValence M K Ndensendo

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Methods Mentioned

BETA
X-ray

Software Mentioned

HyperChem
AutoDock
Hyper Chem
Lig Plot
LigPlot
Discovery studio

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