Glabridin-chalcone hybrid molecules: drug resistance reversal agent against clinical isolates of methicillin-resistantStaphylococcus aureus

MedChemComm
2016.0

Abstract

A novel series of glabridin-chalcone hybrid molecules (GCHMs) were synthesized, evaluated for their antibacterial and resistance reversal activity against clinical isolates of methicillin resistant strain of Staphylococcus aureus (MRSA) alone and in combination with norfloxacin. Glabridin showed significant anti-staphylococcal activity against various MRSA clinical isolates with MICs 12.5 µg/ml. However, all its synthesized derivatives displayed moderate to weak activity (MICs ranging from 12.5- >100 µg/ml). Among all the synthesized hybrid molecules, compounds 6f, 6h, 8f and 8h along with glabridin were chosen for combination study with norfloxacin. Among all tested compounds, 8h exhibited marked synergism up to 16 folds reduction in MICs with norfloxacin (FICI range from 0.312-0.375). In systemically infected Swiss albino mice model, compound 8h significantly (p<0.01, p<0.05) lowered the systemic bacterial load in blood, liver, kidney, lung and spleen tissues. The present study reports the potential use of GCHMs in the development of economical anti-infective combinations for treatment of infection caused by clinical MRSA isolates.

Knowledge Graph

Similar Paper

Glabridin-chalcone hybrid molecules: drug resistance reversal agent against clinical isolates of methicillin-resistantStaphylococcus aureus
MedChemComm 2016.0
Synthesis and anti Methicillin resistant Staphylococcus aureus activity of substituted chalcones alone and in combination with non-beta-lactam antibiotics
Bioorganic &amp; Medicinal Chemistry Letters 2012.0
Novel chalcone-conjugated, multi-flexible end-group coumarin thiazole hybrids as potential antibacterial repressors against methicillin-resistant Staphylococcus aureus
European Journal of Medicinal Chemistry 2021.0
Novel Chalcone–Thiazole Hybrids as Potent Inhibitors of Drug ResistantStaphylococcus aureus
ACS Medicinal Chemistry Letters 2015.0
Synthesis of new chalcone derivatives containing a rhodanine-3-acetic acid moiety with potential anti-bacterial activity
European Journal of Medicinal Chemistry 2010.0
Antibacterial activity of chalcones, hydrazones and oxadiazoles against methicillin-resistant Staphylococcus aureus
Bioorganic &amp; Medicinal Chemistry Letters 2012.0
Synthesis and antibacterial evaluation of rhodanine-based 5-aryloxy pyrazoles against selected methicillin resistant and quinolone-resistant Staphylococcus aureus (MRSA and QRSA)
European Journal of Medicinal Chemistry 2013.0
Synergistic effects of berberines with antibiotics on clinical multi-drug resistant isolates of methicillin-resistant Staphylococcus aureus (MRSA)
Medicinal Chemistry Research 2014.0
Anti-methicillin resistant Staphylococcus aureus activity, synergism with oxacillin and molecular docking studies of metronidazole-triazole hybrids
European Journal of Medicinal Chemistry 2016.0
Bromomethylthioindole Inspired Carbazole Hybrids as Promising Class of Anti-MRSA Agents
ACS Medicinal Chemistry Letters 2016.0