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The vancomycin resistant target enzymes VanX inhibitors and metallo-β- lactamase enzyme assays the reagents Nitrocefin the Synthesis and Characterization

Author: ChengXu
Tutor: YangKeWu
School: Northwestern University
Course: Organic Chemistry
Keywords: Vancomycin-resistant VanX Inhibitors Phosphonamide Nitrocefin
CLC: TQ460.1
Type: Master's thesis
Year: 2011
Downloads: 60
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Abstract


Led with the extensive use of the glycopeptide antibiotic vancomycin , vancomycin-resistant Gram-positive bacteria , particularly Staphylococcus aureus serious threat to human life and health of the phenomenon . The study found that the vancomycin-resistant bacterial D- alanyl -D- alanine (D-Ala-D-Ala) of dipeptide hydrolase VanX in vancomycin resistance plays an important role , is a potential drug targets . Therefore , D-Ala-D-Ala analogs VanX inhibitor study model . By multi-step reaction synthesis of the important intermediate compound methyl 1 - (benzyloxy -carbonyl amide group ) ethyl phosphonate with a variety of amino acid methyl ester of a nucleophilic substitution reaction , to give five kinds of the terminal group protected amino phosphonate compounds . By catalytic hydrogenolysis and the removal of alkaline hydrolysis end base protection groups , the 5 types of D-Ala-D-Ala phosphine lactam inhibitor using 1H NMR , 13C NMR , 31P NMR , IR and MS its characterization . Evaluation of biological activity on the product through the MIC experiments results show that resistant Staphylococcus aureus , after adding compound 6a MIC values ??than just added to the vancomycin MIC values ??8 fold lower , which shows the compound 6a resistant Staphylococcus aureus has a higher inhibitory activity . Resistant MRSA1 and MRSA2 only has a certain degree of inhibitory activity of compound 6a of MRSA2 its MIC value added to the vancomycin MIC values ??compared to only 2-fold lower . Design Synthesis of vancomycin-resistant target enzyme VanX substrate of D-leucine -p- nitroaniline , and D-leucine -p- nitroaniline was determined by ultraviolet spectrometer maximum absorption peak at 258 nm . This article was obtained by the three - step reaction synthesis of β- lactamase detection reagent ceph nitrothieno , and was measured with UV-Vis spectroscopy before and after the action of the metallo-β- lactamase L1 , results showed that , nitrocefin with L1 role , the largest electronic absorption peak shift from 390 nm to 486 nm . As a substrate for the enzyme , cephalosporin nitrothieno can be used for the detection of β- lactamases resistant bacteria .

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