Back to Search
Start Over
The synthesis and antibacterial activity of pyrazole-fused tricyclic diterpene derivatives
- Source :
- European Journal of Medicinal Chemistry. 90:10-20
- Publication Year :
- 2015
- Publisher :
- Elsevier BV, 2015.
-
Abstract
- The diterpenoid compound 5 was identified as an antibacterial lead in our screening of small synthetic natural product-like (NPL) library. A series of novel diterpene derivatives were synthesized and investigated for their activity against Staphylococcus aureus Newman strain and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108 and NRS-271). Among the compounds tested, 42 and 43 showed highest activity with a MIC of 1 μg/mL against strain Newman, 45 and 52 showed the most potent activity with MIC values of 0.71–3.12 μg/mL against five multidrug-resistant S . aureus . All high-antimicrobial active compounds showed no obvious toxicity to human fibroblast (HAF) cells at the MIC concentration.
- Subjects :
- Models, Molecular
Staphylococcus aureus
Stereochemistry
Microbial Sensitivity Tests
Pyrazole
Crystallography, X-Ray
medicine.disease_cause
Structure-Activity Relationship
chemistry.chemical_compound
Drug Resistance, Multiple, Bacterial
Drug Discovery
medicine
Humans
Pharmacology
chemistry.chemical_classification
Dose-Response Relationship, Drug
Molecular Structure
Strain (chemistry)
Organic Chemistry
General Medicine
Fibroblasts
humanities
Terpenoid
Anti-Bacterial Agents
Multiple drug resistance
chemistry
Pyrazoles
Diterpenes
Diterpene
Antibacterial activity
human activities
Tricyclic
Subjects
Details
- ISSN :
- 02235234
- Volume :
- 90
- Database :
- OpenAIRE
- Journal :
- European Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....d2397bdbc8b98ecc2a90120f752301b8