Synthesis and characterization of new Schiff-bases as Methicillin resistant Staphylococcus aureus (MRSA) inhibitors

Methicillin-resistant Staphylococcus aureus (MRSA) is the most common and widespread antibioticresistant species. Novel Schiff-bases (2-8) have been synthesized and characterized using FTIR, H-1 NMR, C-13 NMR and ESI-Mass spectroscopy. An in vitro anti-MRSA study with the ATCC 43300 strain revealed that compounds 2, 4 and 6 inhibited the MRSA strain significantly (MIC 256-512 mu g/mL). The molecular docking study against the FabI enzyme from S. aureus indicated that potent compound 6 has significant docking score (-8.756 Kcal/mol) and forms hydrogen bonding and pi-pi stacking with Tyr157 and additional hydrogen bond with Ser197. All the tested derivatives showed lower toxicity with IC50 values >278 mu M and none of them were cytotoxic against mammalian Vero cell line. (C) 2021 Elsevier B.V. All rights reserved.

Automated summary

Novel Schiff-bases were synthesized and tested for their potential anti-MRSA activity, with compounds 2, 4 and 6 showing significant inhibition against the MRSA strain. Molecular docking studies revealed that compound 6 had strong docking ability against the FabI enzyme from S. aureus. The tested derivatives demonstrated low toxicity and no cytotoxic effects on mammalian cells.