Abstract
Background: Compounds containing CN3 groups are named as guanidine derivatives, which have a rich history in biological and bio-inspired activity. Many guanidine moieties are reported for the antimicrobial activity. Present study aims to the enhancement of bio-activity of the guanidine subunits by conjugating with benzothiazole.
Methods: A new series of benzothiazole guanidines have been synthesized from the reaction of thiourea derivatives of 6-substituted benzothiazoles with different substituted anilines in presence of HgCl2. The synthesized compounds were characterized through FT-IR, mass and 1H NMR spectral techniques. The synthesized compounds were screened for the Antimicrobial activity by disc diffusion method and antioxidant activity was assigned by DPPH and ABTS assay.
Results: The products were screened for antimicrobial activity. They were found to exhibit moderate to potent activity against the tested microorganisms and have shown minimum inhibition concentration of 1.56 µg/mL for Candida albicans, 0.78 µg/mL for Aspergillus niger, 25 µg/mL for S. aureus and 12.5 µg/mL for E. coli. The derivatives were also tested for antioxidant DPPH and ABTS assays and they were found to have significant activities compared to the standards.
Conclusion: In the present work, a new series of benzothiazole guanidinyl derivatives were synthesized in good yields by employing HgCl2 reagent. Synthesized compounds were screened for antimicrobial and antioxidant activities and compounds containing p-methoxy, o-hydroxy showed better antioxidant activities and antimicrobial activities.
Keywords: Benzothiazolyl guanidine, antimicrobial activity, DPPH assay, ABTS assay, antioxidant, Aspergillus niger.
Graphical Abstract
The Natural Products Journal
Title:Synthesis of Benzothiazolyl Guanidinyl Derivatives and their In-Vitro Antimicrobial and Antioxidant Activity
Volume: 7 Issue: 4
Author(s): Mahesh Bhat*, S. L. Belagali and D. C. Shyamala
Affiliation:
- Environmental Chemistry Laboratory, Department of Studies in Environmental Science, University of Mysore, Mysuru- 570 006, Karnataka,India
Keywords: Benzothiazolyl guanidine, antimicrobial activity, DPPH assay, ABTS assay, antioxidant, Aspergillus niger.
Abstract: Background: Compounds containing CN3 groups are named as guanidine derivatives, which have a rich history in biological and bio-inspired activity. Many guanidine moieties are reported for the antimicrobial activity. Present study aims to the enhancement of bio-activity of the guanidine subunits by conjugating with benzothiazole.
Methods: A new series of benzothiazole guanidines have been synthesized from the reaction of thiourea derivatives of 6-substituted benzothiazoles with different substituted anilines in presence of HgCl2. The synthesized compounds were characterized through FT-IR, mass and 1H NMR spectral techniques. The synthesized compounds were screened for the Antimicrobial activity by disc diffusion method and antioxidant activity was assigned by DPPH and ABTS assay.
Results: The products were screened for antimicrobial activity. They were found to exhibit moderate to potent activity against the tested microorganisms and have shown minimum inhibition concentration of 1.56 µg/mL for Candida albicans, 0.78 µg/mL for Aspergillus niger, 25 µg/mL for S. aureus and 12.5 µg/mL for E. coli. The derivatives were also tested for antioxidant DPPH and ABTS assays and they were found to have significant activities compared to the standards.
Conclusion: In the present work, a new series of benzothiazole guanidinyl derivatives were synthesized in good yields by employing HgCl2 reagent. Synthesized compounds were screened for antimicrobial and antioxidant activities and compounds containing p-methoxy, o-hydroxy showed better antioxidant activities and antimicrobial activities.
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Cite this article as:
Bhat Mahesh *, Belagali S. L. and Shyamala D. C., Synthesis of Benzothiazolyl Guanidinyl Derivatives and their In-Vitro Antimicrobial and Antioxidant Activity, The Natural Products Journal 2017; 7 (4) . https://dx.doi.org/10.2174/2210315507666170530091940
DOI https://dx.doi.org/10.2174/2210315507666170530091940 |
Print ISSN 2210-3155 |
Publisher Name Bentham Science Publisher |
Online ISSN 2210-3163 |
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