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Synthesis, antimicrobial, antioxidant, anti-hemolytic and cytotoxic evaluation of new imidazole-based heterocycles
- Source :
- European journal of medicinal chemistry. 46(5)
- Publication Year :
- 2010
-
Abstract
- In the present work, 1-(5-methyl-2-phenyl-1H-imidazol-4-yl)ethanone 1 was prepared and used as a precursor for the synthesis of new thiazole, arylidiene and coumarin derivatives. The antimicrobial, antioxidant, anti-hemolytic, and cytotoxic activities of new compounds have been screened. Compound 12 showed an excellent antibacterial activity for all the tested bacteria with minimal inhibitory concentration (MIC) ranged between 21.9 and 43.8 μg/mL. While, compounds 2, 8 and 10a were the best antioxidant reagents using the DPPH method. Compounds 6a and 10b proved to exhibit potent antioxidative activity as reflected in the ability to inhibit lipid per-oxidation in rat brain and kidney homogenates and rate erythrocyte hemolysis. Compounds 6a proved to have the highest cytotoxic activity (81.9%) followed by 2, 6c, 7b and 12 using in vitro Ehrlich ascites assay. The details synthetic methods, spectroscopic data and biological results are recorded.
- Subjects :
- Antioxidant
Erythrocytes
DPPH
medicine.medical_treatment
Antineoplastic Agents
Microbial Sensitivity Tests
Chemical synthesis
Hemolysis
Antioxidants
chemistry.chemical_compound
Structure-Activity Relationship
Heterocyclic Compounds
Drug Discovery
medicine
Animals
Thiazole
Antibacterial agent
Cell Proliferation
Pharmacology
Bacteria
Molecular Structure
Organic Chemistry
Imidazoles
Stereoisomerism
General Medicine
Antimicrobial
medicine.disease
Anti-Bacterial Agents
Rats
chemistry
Biochemistry
Drug Screening Assays, Antitumor
Antibacterial activity
Subjects
Details
- ISSN :
- 17683254
- Volume :
- 46
- Issue :
- 5
- Database :
- OpenAIRE
- Journal :
- European journal of medicinal chemistry
- Accession number :
- edsair.doi.dedup.....f861ac646db24206f0fba1443ba66e87