Cyclohexyl amide-based novel bacterial topoisomerase inhibitors with prospective GyrA-binding fragments
| Autor: | Marko Anderluh, Matjaž Weiss, Martina Hrast, Irena Zdovc, Doroteja Novak, Nikola Minovski, Anja Kolarič |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
DNA
Bacterial Staphylococcus aureus medicine.drug_class Microbial Sensitivity Tests 01 natural sciences 03 medical and health sciences chemistry.chemical_compound Bacterial Proteins Amide Drug Discovery Escherichia coli Human Umbilical Vein Endothelial Cells medicine Humans Topoisomerase II Inhibitors DNA Gyrase Inhibitors Escherichia coli Infections 030304 developmental biology Pharmacology 0303 health sciences Drug discovery Hep G2 Cells Staphylococcal Infections Cyclohexanols Anti-Bacterial Agents 0104 chemical sciences Molecular Docking Simulation 010404 medicinal & biomolecular chemistry chemistry Biochemistry DNA Gyrase Pyrazoles Molecular Medicine Topoisomerase-II Inhibitor Topoisomerase inhibitor |
| Zdroj: | Future Medicinal Chemistry. 11:935-945 |
| ISSN: | 1756-8927 1756-8919 |
| DOI: | 10.4155/fmc-2018-0472 |
| Popis: | Aim: Novel bacterial topoisomerase inhibitors (NBTIs) are a promising class of bacterial topoisomerase II inhibitors that are gaining more and more importance mainly because of their excellent antibacterial activity, as well as their lack of cross-resistance to quinolones. Results: Described here is the synthesis and biological evaluation of a tiny series of new virtually assembled NBTIs containing synthetically feasible right-hand side fragments capable of binding the GyrA subunit of the bacterial DNA gyrase–DNA complex. Conclusion: NBTI variants with incorporated 1-phenylpyrazole right-hand side moiety show suitable antibacterial activity against Gram-positive Staphylococcus aureus, with confirmed selectivity over the human topoisomerase IIα enzyme. |
| Databáze: | OpenAIRE |
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