1 / 2

噻 [][] 類、苯噻 [][] 類和三環苯噻 [][] 類化合物之製備及其對黃嘌呤氧化酶抑制效果

噻 [][] 類、苯噻 [][] 類和三環苯噻 [][] 類化合物之製備及其對黃嘌呤氧化酶抑制效果.

vartouhi-hansen
Download Presentation

噻 [][] 類、苯噻 [][] 類和三環苯噻 [][] 類化合物之製備及其對黃嘌呤氧化酶抑制效果

An Image/Link below is provided (as is) to download presentation Download Policy: Content on the Website is provided to you AS IS for your information and personal use and may not be sold / licensed / shared on other websites without getting consent from its author. Content is provided to you AS IS for your information and personal use only. Download presentation by click this link. While downloading, if for some reason you are not able to download a presentation, the publisher may have deleted the file from their server. During download, if you can't get a presentation, the file might be deleted by the publisher.

E N D

Presentation Transcript

  1. 噻[][]類、苯噻[][]類和三環苯噻[][]類化合物之製備及其對黃嘌呤氧化酶抑制效果噻[][]類、苯噻[][]類和三環苯噻[][]類化合物之製備及其對黃嘌呤氧化酶抑制效果 • 在先前的研究，我們發現苯類化合物於體外測試有顯著的黃嘌呤氧化抑制活性．2-amino-4H-1,3-benzothiazin-4-one (BJ-6) (IC50 = 5.54μM，Ki = 5.12μM) 以及 4-oxo-4H-1,3-benzothiazinone-2-guanidine (TDW-1) (IC50 = 5.60μM，Ki = 19.47μM)是這一類的代表。於本研究，我們製備一些與苯類的結構有所關聯之化合物，包括類、苯類，和三環的苯類化合物，為了研究其對該酵素的抑制活性，然而，只有tetrazolo [5, 1-b] [1, 3] benzothiazin-9-one (BJ-4)，於200μM濃度時有38.1％的抑制活性，其他則沒有活性。另外，我們以Blois氏方法對自由基清除活性進行測試，發現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)和4-hydrazino-2H-1, 3-benzothiazin-2-one (BJ-702) (IC50=23.14 ±0.01 μM)與α-tocopherol (IC50=24.69 ±0.01 μM)比較，其對DPPH自由基清除具有相當好的活性。

  2. Preparation of Thiazinone, Benzothiazinone and Tricyclic Benzothiazinone Compounds and Evaluation of Their Xanthine • 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).

More Related