| Literature DB >> 29331764 |
Muhammad Taha1, Mastura Arbin2, Norizan Ahmat2, Syahrul Imran2, Fazal Rahim3.
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.Entities:
Keywords: Benzothiazole; SAR; Synthesis; β-Glucuronidase activity
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Year: 2018 PMID: 29331764 DOI: 10.1016/j.bioorg.2018.01.002
Source DB: PubMed Journal: Bioorg Chem ISSN: 0045-2068 Impact factor: 5.275