The Experts below are selected from a list of 273 Experts worldwide ranked by ideXlab platform
Haibin Gong - One of the best experts on this subject based on the ideXlab platform.
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design synthesis and antimicrobial activities of Nitroimidazole derivatives containing 1 3 4 oxadiazole scaffold as fabh inhibitors
Bioorganic & Medicinal Chemistry, 2012Co-Authors: Yao Li, Yang Hu, Shuai Zhang, Haibin GongAbstract:Abstract Nitroimidazoles and their derivatives have drawn continuing interest over the years because of their varied biological activities, recently found application in drug development for antimicrobial chemotherapeutics and antiangiogenic hypoxic cell radiosensitizers. In order to search for novel antibacterial agents, we designed and synthesized a series of secnidazole analogs based on oxadiazole scaffold ( 4 – 21 ). Among these compounds, 4 and 7 – 21 were reported for the first time. These compounds were tested for antibacterial activities against Escherichia coli , Pseudomonas aeruginosa , Bacillus subtilis and Staphylococcus aureus . This new Nitroimidazole derivatives class demonstrated strong antibacterial activities. Escherichia coli β-ketoacyl-acyl carrier protein synthase III (FabH) inhibitory assay and docking simulation indicated that the compounds 2-(2-methoxyphenyl)-5-((2-methyl-5-nitro-1 H -imidazol-1-yl)methyl)-1,3,4-oxadiazole ( 11 ) with MIC of 1.56–3.13 μg/mL against the tested bacterial strains and 2-((2-methyl-5-nitro-1 H -imidazol-1-yl)methyl)-5-(2-methylbenzyl)-1,3,4-oxadiazole ( 12 ) with MIC of 1.56–6.25 μg/mL were most potent inhibitors of Escherichia coli FabH.
Yao Li - One of the best experts on this subject based on the ideXlab platform.
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design synthesis and antimicrobial activities of Nitroimidazole derivatives containing 1 3 4 oxadiazole scaffold as fabh inhibitors
Bioorganic & Medicinal Chemistry, 2012Co-Authors: Yao Li, Yang Hu, Shuai Zhang, Haibin GongAbstract:Abstract Nitroimidazoles and their derivatives have drawn continuing interest over the years because of their varied biological activities, recently found application in drug development for antimicrobial chemotherapeutics and antiangiogenic hypoxic cell radiosensitizers. In order to search for novel antibacterial agents, we designed and synthesized a series of secnidazole analogs based on oxadiazole scaffold ( 4 – 21 ). Among these compounds, 4 and 7 – 21 were reported for the first time. These compounds were tested for antibacterial activities against Escherichia coli , Pseudomonas aeruginosa , Bacillus subtilis and Staphylococcus aureus . This new Nitroimidazole derivatives class demonstrated strong antibacterial activities. Escherichia coli β-ketoacyl-acyl carrier protein synthase III (FabH) inhibitory assay and docking simulation indicated that the compounds 2-(2-methoxyphenyl)-5-((2-methyl-5-nitro-1 H -imidazol-1-yl)methyl)-1,3,4-oxadiazole ( 11 ) with MIC of 1.56–3.13 μg/mL against the tested bacterial strains and 2-((2-methyl-5-nitro-1 H -imidazol-1-yl)methyl)-5-(2-methylbenzyl)-1,3,4-oxadiazole ( 12 ) with MIC of 1.56–6.25 μg/mL were most potent inhibitors of Escherichia coli FabH.
Heinz Schimmel - One of the best experts on this subject based on the ideXlab platform.
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validation of a liquid chromatography tandem mass spectrometry method for the identification and quantification of 5 Nitroimidazole drugs and their corresponding hydroxy metabolites in lyophilised pork meat
Journal of Chromatography A, 2009Co-Authors: Reinhard Zeleny, S Harbeck, Heinz SchimmelAbstract:Abstract A liquid chromatography–electrospray ionisation tandem mass spectrometry method for the simultaneous detection and quantitation of 5-Nitroimidazole veterinary drugs in lyophilised pork meat, the chosen format of a candidate certified reference material, has been developed and validated. Six analytes have been included in the scope of validation, i.e. dimetridazole (DMZ), metronidazole (MNZ), ronidazole (RNZ), hydroxymetronidazole (MNZOH), hydroxyipronidazole (IPZOH), and 2-hydroxymethyl-1-methyl-5-Nitroimidazole (HMMNI). The analytes were extracted from the sample with ethyl acetate, chromatographically separated on a C 18 column, and finally identified and quantified by tandem mass spectrometry in the multiple reaction monitoring mode (MRM) using matrix-matched calibration and 2 H 3 -labelled analogues of the analytes (except for MNZOH, where [ 2 H 3 ]MNZ was used). The method was validated in accordance with Commission Decision 2002/657/EC, by determining selectivity, linearity, matrix effect, apparent recovery, repeatability and intermediate precision, decision limits and detection capabilities, robustness of sample preparation method, and stability of extracts. Recovery at 1 μg/kg level was at 100% (estimates in the range of 101–107%) for all analytes, repeatabilities and intermediate precisions at this level were in the range of 4–12% and 2–9%, respectively. Linearity of calibration curves in the working range 0.5–10 μg/kg was confirmed, with r values typically >0.99. Decision limits (CCα) and detection capabilities (CCβ) according to ISO 11843-2 (calibration curve approach) were 0.29–0.44 and 0.36–0.54 μg/kg, respectively. The method reliably identifies and quantifies the selected Nitroimidazoles in the reconstituted pork meat in the low and sub-μg/kg range and will be applied in an interlaboratory comparison for determining the mass fraction of the selected Nitroimidazoles in the candidate reference material currently developed at IRMM.
Shuai Zhang - One of the best experts on this subject based on the ideXlab platform.
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design synthesis and antimicrobial activities of Nitroimidazole derivatives containing 1 3 4 oxadiazole scaffold as fabh inhibitors
Bioorganic & Medicinal Chemistry, 2012Co-Authors: Yao Li, Yang Hu, Shuai Zhang, Haibin GongAbstract:Abstract Nitroimidazoles and their derivatives have drawn continuing interest over the years because of their varied biological activities, recently found application in drug development for antimicrobial chemotherapeutics and antiangiogenic hypoxic cell radiosensitizers. In order to search for novel antibacterial agents, we designed and synthesized a series of secnidazole analogs based on oxadiazole scaffold ( 4 – 21 ). Among these compounds, 4 and 7 – 21 were reported for the first time. These compounds were tested for antibacterial activities against Escherichia coli , Pseudomonas aeruginosa , Bacillus subtilis and Staphylococcus aureus . This new Nitroimidazole derivatives class demonstrated strong antibacterial activities. Escherichia coli β-ketoacyl-acyl carrier protein synthase III (FabH) inhibitory assay and docking simulation indicated that the compounds 2-(2-methoxyphenyl)-5-((2-methyl-5-nitro-1 H -imidazol-1-yl)methyl)-1,3,4-oxadiazole ( 11 ) with MIC of 1.56–3.13 μg/mL against the tested bacterial strains and 2-((2-methyl-5-nitro-1 H -imidazol-1-yl)methyl)-5-(2-methylbenzyl)-1,3,4-oxadiazole ( 12 ) with MIC of 1.56–6.25 μg/mL were most potent inhibitors of Escherichia coli FabH.
Yang Hu - One of the best experts on this subject based on the ideXlab platform.
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design synthesis and antimicrobial activities of Nitroimidazole derivatives containing 1 3 4 oxadiazole scaffold as fabh inhibitors
Bioorganic & Medicinal Chemistry, 2012Co-Authors: Yao Li, Yang Hu, Shuai Zhang, Haibin GongAbstract:Abstract Nitroimidazoles and their derivatives have drawn continuing interest over the years because of their varied biological activities, recently found application in drug development for antimicrobial chemotherapeutics and antiangiogenic hypoxic cell radiosensitizers. In order to search for novel antibacterial agents, we designed and synthesized a series of secnidazole analogs based on oxadiazole scaffold ( 4 – 21 ). Among these compounds, 4 and 7 – 21 were reported for the first time. These compounds were tested for antibacterial activities against Escherichia coli , Pseudomonas aeruginosa , Bacillus subtilis and Staphylococcus aureus . This new Nitroimidazole derivatives class demonstrated strong antibacterial activities. Escherichia coli β-ketoacyl-acyl carrier protein synthase III (FabH) inhibitory assay and docking simulation indicated that the compounds 2-(2-methoxyphenyl)-5-((2-methyl-5-nitro-1 H -imidazol-1-yl)methyl)-1,3,4-oxadiazole ( 11 ) with MIC of 1.56–3.13 μg/mL against the tested bacterial strains and 2-((2-methyl-5-nitro-1 H -imidazol-1-yl)methyl)-5-(2-methylbenzyl)-1,3,4-oxadiazole ( 12 ) with MIC of 1.56–6.25 μg/mL were most potent inhibitors of Escherichia coli FabH.
