Literature DB >> 29331764

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

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.
Copyright © 2018 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Benzothiazole; SAR; Synthesis; β-Glucuronidase activity

Mesh:

Substances:

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


  3 in total

Review 1.  Therapeutic significance of β-glucuronidase activity and its inhibitors: A review.

Authors:  Paul Awolade; Nosipho Cele; Nagaraju Kerru; Lalitha Gummidi; Ebenezer Oluwakemi; Parvesh Singh
Journal:  Eur J Med Chem       Date:  2019-12-04       Impact factor: 6.514

2.  Bioinformatics: A rational combine approach used for the identification and in-vitro activity evaluation of potent β-Glucuronidase inhibitors.

Authors:  Maria Yousuf; Nimra Naveed Shaikh; Zaheer Ul-Haq; M Iqbal Choudhary
Journal:  PLoS One       Date:  2018-12-05       Impact factor: 3.240

3.  Virtual Screening, Synthesis and Biological Evaluation of Streptococcus mutans Mediated Biofilm Inhibitors.

Authors:  Lubna Atta; Ruqaiya Khalil; Khalid Mohammed Khan; Moatter Zehra; Faiza Saleem; Mohammad Nur-E-Alam; Zaheer Ul-Haq
Journal:  Molecules       Date:  2022-02-21       Impact factor: 4.411

  3 in total

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