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1,2,3-triazole-thiazole hybrids: Synthesis, in vitro antimicrobial activity and antibiofilm studies
- Source :
- Bioorganicmedicinal chemistry letters. 33
- Publication Year :
- 2020
-
Abstract
- A new series of triazole-thiazole hybrids were designed, synthesized by the Multi-component reaction approach and evaluated in vitro antimicrobial activity. Most of the tested series of compounds exhibited promising inhibitory activity against the bacterial strains with values in the range of 2.8 to 15.7 µM. The compounds 8i-8l and 8r showed potential-Candida activity against various Candida strains with spectrum values in the range 5.9–14.2 µM. Further, anti-biofilm and toxicity profiles for the potent compounds were also tested, and it was observed that the compounds 8i, 8k, and 8l were found to inhibit the biofilm formation with IC50 values of 6.6, 16.6 and 15.9 µM, respectively against Bacillus subtilis MTCC 121. Besides, 8k and 8l also displayed promising biofilm formation inhibitory activity towards Staphylococcus aureus MTCC 96 with IC50 values of 13.5 and 12.0 µM respectively. In summary, the activity results has emphasized the compounds 8k and 8l as potential leads for further development of antibacterial, anti-Candida, and anti-biofilm agents.
- Subjects :
- Staphylococcus aureus
1,2,3-Triazole
Antifungal Agents
Clinical Biochemistry
Pharmaceutical Science
Bacillus subtilis
Microbial Sensitivity Tests
medicine.disease_cause
01 natural sciences
Biochemistry
chemistry.chemical_compound
Structure-Activity Relationship
Drug Discovery
medicine
Thiazole
Molecular Biology
Candida
biology
Dose-Response Relationship, Drug
Molecular Structure
010405 organic chemistry
Organic Chemistry
Biofilm
Triazoles
biology.organism_classification
Antimicrobial
In vitro
0104 chemical sciences
Anti-Bacterial Agents
010404 medicinal & biomolecular chemistry
Thiazoles
chemistry
Biofilms
Click chemistry
Molecular Medicine
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 33
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....d62b7057b234496ed6f4d1f56dfc1717