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Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates
- Source :
- European Journal of Medicinal Chemistry. 143:1524-1534
- Publication Year :
- 2018
- Publisher :
- Elsevier BV, 2018.
-
Abstract
- A set of 1,2,3-triazole incorporated quinolone antibiotic conjugates 10–15, 17–19 were synthesized via microwave assisted click chemistry technique. Some of the aryl-substituted conjugates 17–19 show promising antibacterial properties against the tested Gram-positive (S. aureus and S. pyogenes) and Gram-negative bacteria (S. typhi) with potency higher than that of the parent antibiotics 1–3. 2D-QSAR modeling supports the observed biological properties.
- Subjects :
- Quantitative structure–activity relationship
1,2,3-Triazole
medicine.drug_class
Antibiotics
Triazole
Quantitative Structure-Activity Relationship
Chemistry Techniques, Synthetic
Microbial Sensitivity Tests
Quinolones
010402 general chemistry
01 natural sciences
chemistry.chemical_compound
Quinolone antibiotic
Drug Discovery
medicine
Organic chemistry
Pharmacology
Bacteria
biology
010405 organic chemistry
Chemistry
Organic Chemistry
General Medicine
Triazoles
Quinolone
biology.organism_classification
Combinatorial chemistry
Anti-Bacterial Agents
0104 chemical sciences
Click chemistry
Subjects
Details
- ISSN :
- 02235234
- Volume :
- 143
- Database :
- OpenAIRE
- Journal :
- European Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....49e0ecc501011eaf2b40e747271cf469
- Full Text :
- https://doi.org/10.1016/j.ejmech.2017.10.042