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Novel Tetrazole-Based Antimicrobial Agents Targeting Clinical Bacteria Strains: Exploring the Inhibition of Staphylococcus aureus DNA Topoisomerase IV and Gyrase
- Source :
- International Journal of Molecular Sciences; Volume 23; Issue 1; Pages: 378, International Journal of Molecular Sciences, International Journal of Molecular Sciences, Vol 23, Iss 378, p 378 (2022)
- Publication Year :
- 2021
- Publisher :
- Multidisciplinary Digital Publishing Institute, 2021.
-
Abstract
- Eleven novel imide-tetrazoles were synthesized. In the initial stage of research, in silico structure-based pharmacological prediction was conducted. All compounds were screened for antimicrobial activity using standard and clinical strains. Within the studied group, compounds 1–3 were recognized as leading structures with the most promising results in antimicrobial studies. Minimal inhibitory concentration values for compounds 1, 2, 3 were within the range of 0.8–3.2 μg/mL for standard and clinical Gram-positive and Gram-negative bacterial strains, showing in some cases higher activity than the reference Ciprofloxacin. Additionally, all three inhibited the growth of all clinical Staphylococci panels: Staphylococcus aureus (T5592; T5591) and Staphylococcus epidermidis (5253; 4243) with MIC values of 0.8 μg/mL. Selected compounds were examined in topoisomerase IV decatenation assay and DNA gyrase supercoiling assay, followed by suitable molecular docking studies to explore the possible binding modes. In summary, the presented transition from substrate imide-thioureas to imide-tetrazole derivatives resulted in significant increase of antimicrobial properties. The compounds 1–3 proposed here provide a promising basis for further exploration towards novel antimicrobial drug candidates.
- Subjects :
- DNA Topoisomerase IV
Staphylococcus aureus
QH301-705.5
gyrase
Proton Magnetic Resonance Spectroscopy
Tetrazoles
Microbial Sensitivity Tests
Catalysis
Article
Inorganic Chemistry
Topoisomerase II Inhibitors
Physical and Theoretical Chemistry
Biology (General)
Molecular Biology
QD1-999
Spectroscopy
tetrazole
topoisomerase
Organic Chemistry
General Medicine
Computer Science Applications
Anti-Bacterial Agents
Molecular Docking Simulation
Chemistry
antibacterial
DNA Gyrase
antimicrobial
Subjects
Details
- Language :
- English
- ISSN :
- 14220067
- Database :
- OpenAIRE
- Journal :
- International Journal of Molecular Sciences; Volume 23; Issue 1; Pages: 378
- Accession number :
- edsair.doi.dedup.....c4d253f9ba3673d152e21b90c8bae571
- Full Text :
- https://doi.org/10.3390/ijms23010378