Chiral phthalimides against penicillin-binding protein 2a of methicillin-resistant Staphylococcus aureus: molecular docking and in vitro analysis

This study uses three chiral phthalimides (FIA, FIB, and FIC) to check their in silico and in vitro inhibitory effects. Molecular docking of these chiral phthalimides against PBP2a of MRSA was performed initially. After promising results, these novel compounds were screened through the agar-well diffusion method and micro-broth dilution assay to investigate their in vitro inhibitory activities with FIB being the strongest anti-staphylococcal agent yielding a 21 mm zone of inhibition and a minimum inhibitory concentration (MIC) of 0.022 ug, respectively. The zones of inhibition obtained through the in vitro activity showed that these chiral phthalimides possess substantial anti-MRSA activities and have the potential to be considered as alternative chemotherapeutics to treat the infections caused by MRSA after the confirmation of their cytotoxic and pharmacokinetic studies.
Source: Frontiers in Pharmacology - Category: Drugs & Pharmacology Source Type: research