Synthesis: Small library of hybrid scaffolds of benzothiazole having hydrazone and evaluation of their β-glucuronidase activity
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 compoun...
| Published in: | Bioorganic Chemistry |
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| Main Author: | |
| Format: | Article |
| Language: | English |
| Published: |
Academic Press Inc.
2018
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| Online Access: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-85040336943&doi=10.1016%2fj.bioorg.2018.01.002&partnerID=40&md5=9227c9c6d5b8595109fb377272a53c00 |
| Summary: | 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. © 2018 Elsevier Inc. |
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| ISSN: | 452068 |
| DOI: | 10.1016/j.bioorg.2018.01.002 |