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Novel tricyclics (e.g., GSK945237) as potent inhibitors of bacterial type IIA topoisomerases
- Source :
- Bioorganic & Medicinal Chemistry Letters. 26:2464-2469
- Publication Year :
- 2016
- Publisher :
- Elsevier BV, 2016.
-
Abstract
- During the course of our research on the lead optimisation of the NBTI (Novel Bacterial Type II Topoisomerase Inhibitors) class of antibacterials, we discovered a series of tricyclic compounds that showed good Gram-positive and Gram-negative potency. Herein we will discuss the various subunits that were investigated in this series and report advanced studies on compound 1 (GSK945237) which demonstrates good PK and in vivo efficacy properties.
- Subjects :
- 0301 basic medicine
ERG1 Potassium Channel
medicine.drug_class
030106 microbiology
Clinical Biochemistry
Antibiotics
Drug Evaluation, Preclinical
Pharmaceutical Science
Chemistry Techniques, Synthetic
Isomerase
Pharmacology
Gram-Positive Bacteria
Heterocyclic Compounds, 4 or More Rings
Biochemistry
Pneumococcal Infections
03 medical and health sciences
Dogs
In vivo
Drug Discovery
medicine
Animals
Topoisomerase II Inhibitors
Potency
Respiratory Tract Infections
Molecular Biology
chemistry.chemical_classification
Gram-Negative Anaerobic Bacteria
biology
Chemistry
Topoisomerase
Organic Chemistry
Anti-Bacterial Agents
Rats
DNA Topoisomerases, Type II
030104 developmental biology
biology.protein
Molecular Medicine
Heterocyclic Compounds, 3-Ring
Type II topoisomerase
Tricyclic
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 26
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....9f67eb26144e4e029d7a0d4e17988e6f