BIOMAT Database Logo BIOMAT Database Logo

Design, synthesis and antibacterial evaluation of novel AHL analogues. 2013

Jing-Li Ren, and En Zhang, and Xian-Wei Ye, and Meng-Meng Wang, and Bin Yu, and Wen-Hua Wang, and Ya-Zhuo Guo, and Hong-Min Liu
School of Pharmaceutical Sciences and New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, PR China.

Two series of novel AHL analogues were designed, synthesized and evaluated for antibacterial activity under cell membrane conditions in vitro. Analogues 4a-c and 4g-m presented potent activity against Gram-positive bacteria. Especially the analogue 4l exerted the most potent inhibition against Bacillus subtilis with MIC50 value of 1.443μg/ml. To our surprise, analogues 6a-c and 6g showed weak inhibition against Gram-negative bacteria with MIC50 values ranging from 17.589 to 67.840μg/ml. This was the first report about synthesis and antibacterial evaluation in vitro of AHL analogues containing dithioester linkage.

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
D002219 Carbamates Derivatives of carbamic acid, H2NC( Carbamate,Aminoformic Acids,Carbamic Acids,Acids, Aminoformic,Acids, Carbamic
D006090 Gram-Negative Bacteria Bacteria which lose crystal violet stain but are stained pink when treated by Gram's method. Gram Negative Bacteria
D006094 Gram-Positive Bacteria Bacteria which retain the crystal violet stain when treated by Gram's method. Gram Positive Bacteria
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
D015107 4-Butyrolactone One of the FURANS with a carbonyl thereby forming a cyclic lactone. It is an endogenous compound made from gamma-aminobutyrate and is the precursor of gamma-hydroxybutyrate. It is also used as a pharmacological agent and solvent. 1,4-Butanolide,4-Hydroxybutyric Acid Lactone,Furanone, tetrahydro-2-,gamma-Butyrolactone,Dihydro-2(3H)-furanone,1,4 Butanolide,4 Butyrolactone,4 Hydroxybutyric Acid Lactone,Furanone, tetrahydro 2,Lactone, 4-Hydroxybutyric Acid,gamma Butyrolactone
D015195 Drug Design The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include PHARMACOKINETICS, dosage analysis, or drug administration analysis. Computer-Aided Drug Design,Computerized Drug Design,Drug Modeling,Pharmaceutical Design,Computer Aided Drug Design,Computer-Aided Drug Designs,Computerized Drug Designs,Design, Pharmaceutical,Drug Design, Computer-Aided,Drug Design, Computerized,Drug Designs,Drug Modelings,Pharmaceutical Designs
D053038 Quorum Sensing A phenomenon where microorganisms communicate and coordinate their behavior by the accumulation of signaling molecules. A reaction occurs when a substance accumulates to a sufficient concentration. This is most commonly seen in bacteria. Quorum Quenching,Quenching, Quorum,Quenchings, Quorum,Quorum Quenchings,Sensing, Quorum

Related Publications

Jing-Li Ren, and En Zhang, and Xian-Wei Ye, and Meng-Meng Wang, and Bin Yu, and Wen-Hua Wang, and Ya-Zhuo Guo, and Hong-Min Liu
Novel fluoroquinolones analogues bearing 4-(arylcarbamoyl)benzyl: design, synthesis, and antibacterial evaluation.
July 2023, Molecular diversity,
Jing-Li Ren, and En Zhang, and Xian-Wei Ye, and Meng-Meng Wang, and Bin Yu, and Wen-Hua Wang, and Ya-Zhuo Guo, and Hong-Min Liu
Novel analogues of sydnone: synthesis, characterization and antibacterial evaluation.
August 2004, Archiv der Pharmazie,
Jing-Li Ren, and En Zhang, and Xian-Wei Ye, and Meng-Meng Wang, and Bin Yu, and Wen-Hua Wang, and Ya-Zhuo Guo, and Hong-Min Liu
Design, synthesis, and evaluation of novel ethambutol analogues.
March 2008, Bioorganic & medicinal chemistry letters,
Jing-Li Ren, and En Zhang, and Xian-Wei Ye, and Meng-Meng Wang, and Bin Yu, and Wen-Hua Wang, and Ya-Zhuo Guo, and Hong-Min Liu
Design, synthesis and fungicidal evaluation of novel pyraclostrobin analogues.
February 2018, Bioorganic & medicinal chemistry,
Jing-Li Ren, and En Zhang, and Xian-Wei Ye, and Meng-Meng Wang, and Bin Yu, and Wen-Hua Wang, and Ya-Zhuo Guo, and Hong-Min Liu
Design, synthesis and antibacterial activity of novel 1,3-thiazolidine pyrimidine nucleoside analogues.
November 2006, Bioorganic & medicinal chemistry,
Jing-Li Ren, and En Zhang, and Xian-Wei Ye, and Meng-Meng Wang, and Bin Yu, and Wen-Hua Wang, and Ya-Zhuo Guo, and Hong-Min Liu
Design, synthesis and biological evaluation of novel fluorinated docetaxel analogues.
February 2009, European journal of medicinal chemistry,
Jing-Li Ren, and En Zhang, and Xian-Wei Ye, and Meng-Meng Wang, and Bin Yu, and Wen-Hua Wang, and Ya-Zhuo Guo, and Hong-Min Liu
Novel promising linezolid analogues: rational design, synthesis and biological evaluation.
November 2013, European journal of medicinal chemistry,
Jing-Li Ren, and En Zhang, and Xian-Wei Ye, and Meng-Meng Wang, and Bin Yu, and Wen-Hua Wang, and Ya-Zhuo Guo, and Hong-Min Liu
Design, synthesis and evaluation of a series of novel fumagillin analogues.
November 2003, Bioorganic & medicinal chemistry,
Jing-Li Ren, and En Zhang, and Xian-Wei Ye, and Meng-Meng Wang, and Bin Yu, and Wen-Hua Wang, and Ya-Zhuo Guo, and Hong-Min Liu
Design, synthesis and evaluation of biological activity of novel fasudil analogues.
December 2014, Die Pharmazie,
Jing-Li Ren, and En Zhang, and Xian-Wei Ye, and Meng-Meng Wang, and Bin Yu, and Wen-Hua Wang, and Ya-Zhuo Guo, and Hong-Min Liu
Design, Synthesis and Anticancer Evaluation of Novel Series of Indibulin Analogues.
January 2019, Medicinal chemistry (Shariqah (United Arab Emirates)),
Copied contents to your clipboard!