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Synthesis: Small library of hybrid scaffolds of benzothiazole having hydrazone and evaluation of their β-glucuronidase activity
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2018-01-04 , DOI: 10.1016/j.bioorg.2018.01.002
Muhammad Taha , Mastura Arbin , Norizan Ahmat , Syahrul Imran , Fazal Rahim

Due to the great biological importance of β-glucuronidase inhibitors, here in this study, we have synthesized a library of novel benzothiazole derivatives (130), characterized by different spectroscopic methods and evaluated for β-glucuronidase inhibitory potential. Among the series sixteen compounds i.e. 16, 8, 9, 11, 14, 15, 2023 and 26 showed outstanding inhibitory potential with IC50 value ranging in between 16.50 ± 0.26 and 59.45 ± 1.12 when compared with standard d-Saccharic acid 1,4-lactone (48.4 ± 1.25 µM). Except compound 8 and 23 all active analogs showed better potential than the standard. Structure activity relationship has been established.



中文翻译:

合成:具有的苯并噻唑杂化支架小文库及其β-葡萄糖醛酸苷酶活性的评估

由于大生物重要性β葡糖醛酸酶抑制剂,这里在本研究中,我们已经合成了新颖的苯并噻唑衍生物(库1 - 30),其特征在于由不同的光谱方法和评价β葡萄糖醛酸酶抑制潜力。间的系列16个的化合物,即 1 - 68911141520 - 2326显示出杰出的抑制潜力与IC 50与标准d-蔗糖酸1,4-内酯(48.4±1.25 µM)相比,该值在16.50±0.26和59.45±1.12之间。除化合物823外,所有活性类似物均显示出比标准品更好的电势。已建立结构活动关系。

更新日期:2018-01-04
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