| Summary: | 碩士 === 台北醫學院 === 藥學研究所 === 87 === In a previous study, we found that benzothiazinone compounds displayed a significant inhibition on xanthine oxidase in in vitro test. 2-Amino-4H-1,3-benzothiazin-4-one (BJ-6) (IC50 = 5.54μM, Ki = 5.12μM) and 4-oxo-4H-1,3-benzothiazinone-2-guanidine (TDW-1) (IC50 = 5.60μM, Ki = 19.47μM) are the representatives of this class.
In this study, we prepared several thiazinone analogues, benzothiazinone analogues, and tricyclic benzothiazinones that are structurally related to the benzothiazinone in order to search for the pharmacophore for enzyme inhibition. However, we found that only tetrazolo [5, 1-b] [1, 3] benzothiazin-9-one (BJ-4) is the compound showed 38.1% xanthine oxidase inhibition at 200μM level, others were apparently inactive.
In addition, we also clarified the free radical scavenging activity of these compounds by virtue of Blois method, we found 2-hydrazino-4H-1, 3-benzothiazin-4-one (BJ-3) (IC50 = 23.29 ± 0.02 μM), 4-hydrazino-2H-1, 3-benzothiazin-2-thione (BJ-5) (IC50 = 19.60 ± 0.02 μM) and 4-hydrazino-2H-1, 3-benzothiazin-2-one (BJ-702) (IC50 = 23.14 ± 0.01 μM) showed DPPH free radical scavenging activity comparable to that of α-tocopherol (IC50 = 24.69 ± 0.01 μM).
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