Synthesis and bioactivity evaluation of rhodanine derivatives as potential anti-bacterial agents. 2012

Ming-Xia Song, and Chang-Ji Zheng, and Xian-Qing Deng, and Qing Wang, and Shao-Pu Hou, and Ting-Ting Liu, and Xiao-Lan Xing, and Hu-Ri Piao
Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University, College of Pharmacy, Yanji City, Jilin Province 133002, PR China.

Five series of (Z)-5-(4-(2-oxo-2-phenylethoxy)benzylidene)-2-thioxothiazolidin-4-one derivatives (I-V) were synthesized, characterized, and evaluated for their anti-bacterial activity. Most of the synthesized compounds showed potent inhibition against several Gram-positive bacteria (including multidrug-resistant clinical isolates) with MIC values in the range of 1-32 μg/mL. Compounds IIIi, Vb and Vc presented the most potent activity, showing four-fold more potency than norfloxacin (MIC = 8 μg/mL and 4 μg/mL) and 64-fold more activity than oxacillin (MIC > 64 μg/mL) against MRSA CCARM 3167 and 3506 strains with MIC values of 1 μg/mL, and 64-fold more potency than norfloxacin (MIC > 64 μg/mL) and comparable activity to oxacillin (MIC = 1 μg/mL) against the QRSA CCARM 3505 and 3519 strains. None of the compounds exhibited any activity against the Gram-negative bacteria Escherichia coli 1356 at 64 μg/mL.

UI MeSH Term Description Entries
D008826 Microbial Sensitivity Tests Any tests that demonstrate the relative efficacy of different chemotherapeutic agents against specific microorganisms (i.e., bacteria, fungi, viruses). Bacterial Sensitivity Tests,Drug Sensitivity Assay, Microbial,Minimum Inhibitory Concentration,Antibacterial Susceptibility Breakpoint Determination,Antibiogram,Antimicrobial Susceptibility Breakpoint Determination,Bacterial Sensitivity Test,Breakpoint Determination, Antibacterial Susceptibility,Breakpoint Determination, Antimicrobial Susceptibility,Fungal Drug Sensitivity Tests,Fungus Drug Sensitivity Tests,Sensitivity Test, Bacterial,Sensitivity Tests, Bacterial,Test, Bacterial Sensitivity,Tests, Bacterial Sensitivity,Viral Drug Sensitivity Tests,Virus Drug Sensitivity Tests,Antibiograms,Concentration, Minimum Inhibitory,Concentrations, Minimum Inhibitory,Inhibitory Concentration, Minimum,Inhibitory Concentrations, Minimum,Microbial Sensitivity Test,Minimum Inhibitory Concentrations,Sensitivity Test, Microbial,Sensitivity Tests, Microbial,Test, Microbial Sensitivity,Tests, Microbial Sensitivity
D000900 Anti-Bacterial Agents Substances that inhibit the growth or reproduction of BACTERIA. Anti-Bacterial Agent,Anti-Bacterial Compound,Anti-Mycobacterial Agent,Antibacterial Agent,Antibiotics,Antimycobacterial Agent,Bacteriocidal Agent,Bacteriocide,Anti-Bacterial Compounds,Anti-Mycobacterial Agents,Antibacterial Agents,Antibiotic,Antimycobacterial Agents,Bacteriocidal Agents,Bacteriocides,Agent, Anti-Bacterial,Agent, Anti-Mycobacterial,Agent, Antibacterial,Agent, Antimycobacterial,Agent, Bacteriocidal,Agents, Anti-Bacterial,Agents, Anti-Mycobacterial,Agents, Antibacterial,Agents, Antimycobacterial,Agents, Bacteriocidal,Anti Bacterial Agent,Anti Bacterial Agents,Anti Bacterial Compound,Anti Bacterial Compounds,Anti Mycobacterial Agent,Anti Mycobacterial Agents,Compound, Anti-Bacterial,Compounds, Anti-Bacterial
D012236 Rhodanine
D015363 Quinolones A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID. Ketoquinoline,Ketoquinolines,Oxoquinoline,Oxoquinolines,Quinolinone,Quinolinones,Quinolone
D055624 Methicillin-Resistant Staphylococcus aureus A strain of Staphylococcus aureus that is non-susceptible to the action of METHICILLIN. The mechanism of resistance usually involves modification of normal or the presence of acquired PENICILLIN BINDING PROTEINS. MRSA,Methicillin Resistant Staphylococcus aureus
D060326 Chemistry Techniques, Synthetic Methods used for the chemical synthesis of compounds. Included under this heading are laboratory methods used to synthesize a variety of chemicals and drugs. Inorganic Synthesis,Inorganic Synthesis Methods,Inorganic Synthesis Techniques,Methods of Inorganic Synthesis,Methods of Organic Synthesis,Methods of Peptide Synthesis,Organic Synthesis,Organic Synthesis Methods,Organic Synthesis Techniques,Peptide Synthesis Methods,Peptide Synthesis Techniques,Peptide Synthesis, Synthetic,Synthetic Chemistry Techniques,Synthetic Peptide Synthesis,Chemistry Technique, Synthetic,Inorganic Syntheses,Inorganic Synthesis Method,Inorganic Synthesis Technique,Method, Inorganic Synthesis,Method, Organic Synthesis,Method, Peptide Synthesis,Methods, Inorganic Synthesis,Methods, Organic Synthesis,Methods, Peptide Synthesis,Organic Syntheses,Organic Synthesis Technique,Peptide Syntheses, Synthetic,Peptide Synthesis Method,Peptide Synthesis Technique,Syntheses, Inorganic,Syntheses, Organic,Syntheses, Synthetic Peptide,Synthesis Method, Inorganic,Synthesis Method, Peptide,Synthesis Methods, Inorganic,Synthesis Methods, Peptide,Synthesis Technique, Inorganic,Synthesis Technique, Organic,Synthesis Technique, Peptide,Synthesis Techniques, Inorganic,Synthesis Techniques, Organic,Synthesis Techniques, Peptide,Synthesis, Inorganic,Synthesis, Organic,Synthesis, Synthetic Peptide,Synthetic Chemistry Technique,Synthetic Peptide Syntheses,Technique, Inorganic Synthesis,Technique, Organic Synthesis,Technique, Peptide Synthesis,Technique, Synthetic Chemistry,Techniques, Inorganic Synthesis,Techniques, Organic Synthesis,Techniques, Peptide Synthesis,Techniques, Synthetic Chemistry
D018432 Drug Resistance, Multiple Simultaneous resistance to several structurally and functionally distinct drugs. Drug Resistance, Extensively,Extensively Drug Resistance,Extensively-Drug Resistance,Multidrug Resistance,Multi-Drug Resistance,Extensively Drug Resistances,Extensively-Drug Resistances,Multiple Drug Resistance,Resistance, Extensively Drug,Resistance, Extensively-Drug,Resistance, Multiple Drug

Related Publications

Ming-Xia Song, and Chang-Ji Zheng, and Xian-Qing Deng, and Qing Wang, and Shao-Pu Hou, and Ting-Ting Liu, and Xiao-Lan Xing, and Hu-Ri Piao
June 2019, European journal of medicinal chemistry,
Ming-Xia Song, and Chang-Ji Zheng, and Xian-Qing Deng, and Qing Wang, and Shao-Pu Hou, and Ting-Ting Liu, and Xiao-Lan Xing, and Hu-Ri Piao
August 2023, Chemistry & biodiversity,
Ming-Xia Song, and Chang-Ji Zheng, and Xian-Qing Deng, and Qing Wang, and Shao-Pu Hou, and Ting-Ting Liu, and Xiao-Lan Xing, and Hu-Ri Piao
January 2023, Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents,
Ming-Xia Song, and Chang-Ji Zheng, and Xian-Qing Deng, and Qing Wang, and Shao-Pu Hou, and Ting-Ting Liu, and Xiao-Lan Xing, and Hu-Ri Piao
July 2018, MedChemComm,
Ming-Xia Song, and Chang-Ji Zheng, and Xian-Qing Deng, and Qing Wang, and Shao-Pu Hou, and Ting-Ting Liu, and Xiao-Lan Xing, and Hu-Ri Piao
January 2017, Bioorganic & medicinal chemistry letters,
Ming-Xia Song, and Chang-Ji Zheng, and Xian-Qing Deng, and Qing Wang, and Shao-Pu Hou, and Ting-Ting Liu, and Xiao-Lan Xing, and Hu-Ri Piao
June 2017, Molecules (Basel, Switzerland),
Ming-Xia Song, and Chang-Ji Zheng, and Xian-Qing Deng, and Qing Wang, and Shao-Pu Hou, and Ting-Ting Liu, and Xiao-Lan Xing, and Hu-Ri Piao
November 2021, Bioorganic & medicinal chemistry,
Ming-Xia Song, and Chang-Ji Zheng, and Xian-Qing Deng, and Qing Wang, and Shao-Pu Hou, and Ting-Ting Liu, and Xiao-Lan Xing, and Hu-Ri Piao
September 2022, Bioorganic chemistry,
Ming-Xia Song, and Chang-Ji Zheng, and Xian-Qing Deng, and Qing Wang, and Shao-Pu Hou, and Ting-Ting Liu, and Xiao-Lan Xing, and Hu-Ri Piao
October 2016, Bioorganic chemistry,
Ming-Xia Song, and Chang-Ji Zheng, and Xian-Qing Deng, and Qing Wang, and Shao-Pu Hou, and Ting-Ting Liu, and Xiao-Lan Xing, and Hu-Ri Piao
October 2018, International journal of molecular sciences,
Copied contents to your clipboard!