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Synthesis and Biological Evaluation of New Compounds with Nitroimidazole Moiety.
- Source :
-
Molecules (Basel, Switzerland) [Molecules] 2024 Jun 26; Vol. 29 (13). Date of Electronic Publication: 2024 Jun 26. - Publication Year :
- 2024
-
Abstract
- Heterocyclic compounds, particularly those containing azole rings, have shown extensive biological activity, including anticancer, antibacterial, and antifungal properties. Among these, the imidazole ring stands out due to its diverse therapeutic potential. In the presented study, we designed and synthesized a series of imidazole derivatives to identify compounds with high biological potential. We focused on two groups: thiosemicarbazide derivatives and hydrazone derivatives. We synthesized these compounds using conventional methods and confirmed their structures via nuclear magnetic resonance spectroscopy (NMR), MS, and elemental analysis, and then assessed their antibacterial and antifungal activities in vitro using the broth microdilution method against Gram-positive and Gram-negative bacteria, as well as Candida spp. strains. Our results showed that thiosemicarbazide derivatives exhibited varied activity against Gram-positive bacteria, with MIC values ranging from 31.25 to 1000 µg/mL. The hydrazone derivatives, however, did not display significant antibacterial activity. These findings suggest that structural modifications can significantly influence the antimicrobial efficacy of imidazole derivatives, highlighting the potential of thiosemicarbazide derivatives as promising candidates for further development in antibacterial therapies. Additionally, the cytotoxic activity against four cancer cell lines was evaluated. Two derivatives of hydrazide-hydrazone showed moderate anticancer activity.
- Subjects :
- Humans
Nitroimidazoles pharmacology
Nitroimidazoles chemistry
Nitroimidazoles chemical synthesis
Cell Line, Tumor
Gram-Negative Bacteria drug effects
Structure-Activity Relationship
Semicarbazides chemistry
Semicarbazides pharmacology
Semicarbazides chemical synthesis
Hydrazones chemistry
Hydrazones pharmacology
Hydrazones chemical synthesis
Candida drug effects
Molecular Structure
Microbial Sensitivity Tests
Anti-Bacterial Agents pharmacology
Anti-Bacterial Agents chemical synthesis
Anti-Bacterial Agents chemistry
Antineoplastic Agents pharmacology
Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Antifungal Agents pharmacology
Antifungal Agents chemical synthesis
Antifungal Agents chemistry
Gram-Positive Bacteria drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1420-3049
- Volume :
- 29
- Issue :
- 13
- Database :
- MEDLINE
- Journal :
- Molecules (Basel, Switzerland)
- Publication Type :
- Academic Journal
- Accession number :
- 38998972
- Full Text :
- https://doi.org/10.3390/molecules29133023