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Synthesis, antimicrobial, DNA cleavage and antioxidant activities of tricyclic sultams derived from saccharin
- Source :
- European Journal of Medicinal Chemistry. 139:107-113
- Publication Year :
- 2017
- Publisher :
- Elsevier BV, 2017.
-
Abstract
- Two series of fused tricyclic sultams (carboxylates, 3a, b and 5a, f, g and anilides 5b-e) were synthesized from saccharin and their chemical structures were confirmed by spectroscopic tools. Then, their antibacterial activities and MIC were evaluated against two strains of gram positive and gram-negative bacteria. The MIC values of the tested compounds are in the of range 8–33 μg/ml. In addition, their DNA cleavage ability, binding affinity and their anticancer activities against hepatic cancer cell were tested. And their antioxidant activities were also measured. Four carboxylate derivatives ( 3a, 5a, 5f and 5g) and one anilide ( 5d ) of the tested compounds proved to be the highest activity all over the study.
- Subjects :
- Staphylococcus aureus
Antioxidant
Stereochemistry
medicine.medical_treatment
Antineoplastic Agents
Microbial Sensitivity Tests
010402 general chemistry
01 natural sciences
Antioxidants
Structure-Activity Relationship
chemistry.chemical_compound
Saccharin
Dna cleavage
Cell Line, Tumor
Drug Discovery
Escherichia coli
medicine
Humans
Carboxylate
DNA Cleavage
Cell Proliferation
Pharmacology
chemistry.chemical_classification
Sulfonamides
Dose-Response Relationship, Drug
Molecular Structure
biology
010405 organic chemistry
Organic Chemistry
General Medicine
biology.organism_classification
Antimicrobial
Anti-Bacterial Agents
0104 chemical sciences
chemistry
Pseudomonas aeruginosa
Cancer cell
Drug Screening Assays, Antitumor
Bacteria
Tricyclic
Subjects
Details
- ISSN :
- 02235234
- Volume :
- 139
- Database :
- OpenAIRE
- Journal :
- European Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....55cced1af664f0aed792323e93e37571
- Full Text :
- https://doi.org/10.1016/j.ejmech.2017.07.079