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

Abstract

With an intention to synergize the anti-bacterial activity of 5-aryloxy pyrazole and rhodanine derivatives, eight series of hybrid compounds have been synthesized and evaluated for their antibacterial activity. The majority of the synthesized compounds showed good inhibitory activity against selected methicillin resistant and quinolone-resistant Staphylococcus aureus (MRSA, QRSA) with minimum inhibitory concentration (MIC) values in the range of 1-32 μg/mL. The cytotoxicity test suggests that these compounds exhibited in vitro antibacterial activity at non-cytotoxic concentrations. These studies therefore suggest that rhodanine-based 5-aryloxy pyrazoles are interesting scaffolds for the development of novel Gram-positive antibacterial agents.

Knowledge Graph

Similar Paper

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
Synthesis and biological evaluation of 5-aryloxypyrazole derivatives bearing a rhodanine-3-aromatic acid as potential antimicrobial agents
Bioorganic & Medicinal Chemistry Letters 2012.0
Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents
Bioorganic & Medicinal Chemistry Letters 2013.0
Synthesis and antibacterial activity of novel 1,3-diphenyl-1H-pyrazoles functionalized with phenylalanine-derived rhodanines
European Journal of Medicinal Chemistry 2012.0
Synthesis and bioactivity evaluation of rhodanine derivatives as potential anti-bacterial agents
European Journal of Medicinal Chemistry 2012.0
Synthesis of novel 1,3-diaryl pyrazole derivatives bearing rhodanine-3-fatty acid moieties as potential antibacterial agents
European Journal of Medicinal Chemistry 2012.0
The synthesis of phenylalanine-derived C5-substituted rhodanines and their activity against selected methicillin-resistant Staphylococcus aureus (MRSA) strains
European Journal of Medicinal Chemistry 2010.0
The synthesis and SAR study of phenylalanine-derived (Z)-5-arylmethylidene rhodanines as anti-methicillin-resistant Staphylococcus aureus (MRSA) compounds
Bioorganic & Medicinal Chemistry Letters 2013.0
Synthesis and potential antibacterial activity of new rhodanine-3-acetic acid derivatives
Medicinal Chemistry Research 2013.0
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety
Bioorganic & Medicinal Chemistry Letters 2015.0