Synthesis: Small library of hybrid scaffolds of benzothiazole having hydrazone and evaluation of their β-glucuronidase activity

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...

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Published in:Bioorganic Chemistry
Main Author: Taha M.; Arbin M.; Ahmat N.; Imran S.; Rahim F.
Format: Article
Language:English
Published: Academic Press Inc. 2018
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
id 2-s2.0-85040336943
spelling 2-s2.0-85040336943
Taha M.; Arbin M.; Ahmat N.; Imran S.; Rahim F.
Synthesis: Small library of hybrid scaffolds of benzothiazole having hydrazone and evaluation of their β-glucuronidase activity
2018
Bioorganic Chemistry
77

10.1016/j.bioorg.2018.01.002
https://www.scopus.com/inward/record.uri?eid=2-s2.0-85040336943&doi=10.1016%2fj.bioorg.2018.01.002&partnerID=40&md5=9227c9c6d5b8595109fb377272a53c00
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.
Academic Press Inc.
452068
English
Article
author Taha M.; Arbin M.; Ahmat N.; Imran S.; Rahim F.
spellingShingle Taha M.; Arbin M.; Ahmat N.; Imran S.; Rahim F.
Synthesis: Small library of hybrid scaffolds of benzothiazole having hydrazone and evaluation of their β-glucuronidase activity
author_facet Taha M.; Arbin M.; Ahmat N.; Imran S.; Rahim F.
author_sort Taha M.; Arbin M.; Ahmat N.; Imran S.; Rahim F.
title Synthesis: Small library of hybrid scaffolds of benzothiazole having hydrazone and evaluation of their β-glucuronidase activity
title_short Synthesis: Small library of hybrid scaffolds of benzothiazole having hydrazone and evaluation of their β-glucuronidase activity
title_full Synthesis: Small library of hybrid scaffolds of benzothiazole having hydrazone and evaluation of their β-glucuronidase activity
title_fullStr Synthesis: Small library of hybrid scaffolds of benzothiazole having hydrazone and evaluation of their β-glucuronidase activity
title_full_unstemmed Synthesis: Small library of hybrid scaffolds of benzothiazole having hydrazone and evaluation of their β-glucuronidase activity
title_sort Synthesis: Small library of hybrid scaffolds of benzothiazole having hydrazone and evaluation of their β-glucuronidase activity
publishDate 2018
container_title Bioorganic Chemistry
container_volume 77
container_issue
doi_str_mv 10.1016/j.bioorg.2018.01.002
url https://www.scopus.com/inward/record.uri?eid=2-s2.0-85040336943&doi=10.1016%2fj.bioorg.2018.01.002&partnerID=40&md5=9227c9c6d5b8595109fb377272a53c00
description 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.
publisher Academic Press Inc.
issn 452068
language English
format Article
accesstype
record_format scopus
collection Scopus
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