Synthesis: Small library of hybrid scaffolds of benzothiazole having hydrazone and evaluation of their β-glucuronidase activity.
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Abstract | :
Due to the great biological importance of β-glucuronidase inhibitors, here in this study, we have synthesized a library of novel benzothiazole derivatives (1-30), characterized by different spectroscopic methods and evaluated for β-glucuronidase inhibitory potential. Among the series sixteen compounds i.e.1-6, 8, 9, 11, 14, 15, 20-23 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. |
Year of Publication | :
2018
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Journal | :
Bioorganic chemistry
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Volume | :
77
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Number of Pages | :
47-55
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Date Published | :
2018
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ISSN Number | :
0045-2068
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URL | :
http://linkinghub.elsevier.com/retrieve/pii/S0045-2068(17)30606-5
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DOI | :
10.1016/j.bioorg.2018.01.002
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Short Title | :
Bioorg Chem
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