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2-Phenyl-5,6-dihydro-2H-thieno[3,2-c]pyrazol-3-ol derivatives as new inhibitors of bacterial cell wall biosynthesis
- Source :
- Bioorganic & Medicinal Chemistry Letters. 13:2591-2594
- Publication Year :
- 2003
- Publisher :
- Elsevier BV, 2003.
-
Abstract
- Twenty-five 2-phenyl-5,6-dihydro-2H-thieno[3,2-c]pyrazol-3-ol derivatives were synthesized for evaluation as new inhibitors of bacterial cell wall biosynthesis. Many of them demonstrated good inhibitory activity against Staphylococcus aureus MurB, MurC and MurD enzymes in vitro and antimicrobial activity against gram-positive bacteria including MRSA, VRE and PRSP. However, when they were tested in the presence of 4% bovine serum albumin, the MIC values increased to greater than 128 microg/mL against PRSP. None of the compounds demonstrated activity against gram-negative bacteria at MIC
- Subjects :
- Staphylococcus aureus
Stereochemistry
Gram-positive bacteria
Clinical Biochemistry
Pharmaceutical Science
Microbial Sensitivity Tests
Gram-Positive Bacteria
medicine.disease_cause
Biochemistry
Bacterial cell structure
Cell Wall
Drug Resistance, Bacterial
Drug Discovery
medicine
Bovine serum albumin
Molecular Biology
Antibacterial agent
chemistry.chemical_classification
biology
Chemistry
Organic Chemistry
biology.organism_classification
Antimicrobial
Anti-Bacterial Agents
Enzyme
Genes, Bacterial
biology.protein
Molecular Medicine
Bacteria
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 13
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....63ed4dae9e41d284502531533dc4ccff