Exploration of the Antimicrobial Effects of Benzothiazolylthiazolidin-4-One and In Silico Mechanistic Investigation Article Swipe
YOU?
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· 2021
· Open Access
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· DOI: https://doi.org/10.3390/molecules26134061
Background: Infectious diseases still affect large populations causing significant morbidity and mortality. Bacterial and fungal infections for centuries were the main factors of death and disability of millions of humans. Despite the progress in the control of infectious diseases, the appearance of resistance of microbes to existing drugs creates the need for the development of new effective antimicrobial agents. In an attempt to improve the antibacterial activity of previously synthesized compounds modifications to their structures were performed. Methods: Nineteen thiazolidinone derivatives with 6-Cl, 4-OMe, 6-CN, 6-adamantan, 4-Me, 6-adamantan substituents at benzothiazole ring were synthesized and evaluated against panel of four bacterial strains S. aureus, L. monocytogenes, E. coli and S. typhimirium and three resistant strains MRSA, E. coli and P. aeruginosa in order to improve activity of previously evaluated 6-OCF3-benzothiazole-based thiazolidinones. The evaluation of minimum inhibitory and minimum bactericidal concentration was determined by microdilution method. As reference compounds ampicillin and streptomycin were used. Results: All compounds showed antibacterial activity with MIC in range of 0.12–0.75 mg/mL and MBC at 0.25–>1.00 mg/mL The most active compound among all tested appeared to be compound 18, with MIC at 0.10 mg/mL and MBC at 0.12 mg/mL against P. aeruginosa. as well as against resistant strain P. aeruginosa with MIC at 0.06 mg/mL and MBC at 0.12 mg/mL almost equipotent with streptomycin and better than ampicillin. Docking studies predicted that the inhibition of LD-carboxypeptidase is probably the possible mechanism of antibacterial activity of tested compounds. Conclusion: The best improvement of antibacterial activity after modifications was achieved by replacement of 6-OCF3 substituent in benzothiazole moiety by 6-Cl against S. aureus, MRSA and resistant strain of E. coli by 2.5 folds, while against L. monocytogenes and S. typhimirium from 4 to 5 folds.
Related Topics
- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.3390/molecules26134061
- https://www.mdpi.com/1420-3049/26/13/4061/pdf?version=1625228905
- OA Status
- gold
- Cited By
- 19
- References
- 66
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W3174662174
Raw OpenAlex JSON
- OpenAlex ID
-
https://openalex.org/W3174662174Canonical identifier for this work in OpenAlex
- DOI
-
https://doi.org/10.3390/molecules26134061Digital Object Identifier
- Title
-
Exploration of the Antimicrobial Effects of Benzothiazolylthiazolidin-4-One and In Silico Mechanistic InvestigationWork title
- Type
-
articleOpenAlex work type
- Language
-
enPrimary language
- Publication year
-
2021Year of publication
- Publication date
-
2021-07-02Full publication date if available
- Authors
-
Michelyne Haroun, Christophe Tratrat, Anthi Petrou, Athina Geronikaki, Marija Ivanov, Ana Ćirić, Marina Sokóvić, Nagaraja Sreeharsha, Katharigatta N. Venugopala, Anroop B. Nair, Heba S. Elsewedy, Hafedh KochkarList of authors in order
- Landing page
-
https://doi.org/10.3390/molecules26134061Publisher landing page
- PDF URL
-
https://www.mdpi.com/1420-3049/26/13/4061/pdf?version=1625228905Direct link to full text PDF
- Open access
-
YesWhether a free full text is available
- OA status
-
goldOpen access status per OpenAlex
- OA URL
-
https://www.mdpi.com/1420-3049/26/13/4061/pdf?version=1625228905Direct OA link when available
- Concepts
-
In silico, Antimicrobial, Computational biology, Biochemical engineering, Chemistry, Biology, Microbiology, Biochemistry, Engineering, GeneTop concepts (fields/topics) attached by OpenAlex
- Cited by
-
19Total citation count in OpenAlex
- Citations by year (recent)
-
2025: 4, 2024: 3, 2023: 5, 2022: 6, 2021: 1Per-year citation counts (last 5 years)
- References (count)
-
66Number of works referenced by this work
- Related works (count)
-
10Other works algorithmically related by OpenAlex
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| publication_date | 2021-07-02 |
| publication_year | 2021 |
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