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Study of a Novel Monoamine Oxidase Fluorogenic Probe and Aryloxycarboxylic Acetamide Inhibitors

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Tutor: Zhu
School: Zhejiang University of Technology
Course: Biochemical Engineering
Keywords: fluorogenic probe,monoamide oxidase,inhibitor,aryloxycarboxylic acetamide
CLC: TQ463
Type: Master's thesis
Year:  2011
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In recent years, as monoamine oxidase structures and mechanism of action were clarified, the study of MAO probe and MAO inhibitor have attracted many attentions. This paper studys the following aspects.First, we synthesized a new novel of fluorogenic probe: 4-methyl-7-(1-methyl-1,2,3,6-tetrahydropyridin-4-yloxy)-coumarin. It has 1, 2, 3, 6-tetrahydropyridin group as a MAO substrates and a coumarin as a fluroscent indicator. By comparing the intensity of the fluorescence before and after the reaction, the activities of MAOs could be easily detected.Then, we synthesized a series of aryloxycarboxylic acetamides and tetrazole analogues which were further evaluated for their monoamine oxidase A and B inhibitory activity.In conclusion, we got a kind of flurorescent probe which has good selectivity, and it could be applied in the high-throughput screening of monoamine oxidase inhitors. The inhibitor experiments showed that aryloxycarboxylic acetamide analogues have good selectivity to monoamine oxidase A. Compounds 2-9 (SI = 245) and compounds 2-13 (SI = 180) have the best selectivity to MAO-A, while compouds 2-23 and 2-25 show the best inhibitory activity against MAO-A and B respectively.But so far, we did not find better MAO inhibitor from the tetrazole compouds. Further modification are needed to find tetrazole compounds with excellent inhibitory activity against MAO-A/B.
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