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DNA gyrase subunit A
A DNA gyrase subunit A that is encoded in the genome of Escherichia coli K-12. [PRO:DNx, UniProtKB:P0AES4]
Synonyms
EC 5.6.2.2
Research
Bioassay Publications (37)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 9 (24.32) | 29.6817 |
| 2010's | 17 (45.95) | 24.3611 |
| 2020's | 11 (29.73) | 2.80 |
Compounds (18)
Drugs with Inhibition Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ciprofloxacin | Escherichia coli K-12 | Activity | 10.7200 | 4 | 4 |
| ciprofloxacin | Escherichia coli K-12 | EC | 1.2000 | 1 | 1 |
| ofloxacin | Escherichia coli K-12 | CC25 | 0.2000 | 1 | 1 |
| moxifloxacin | Escherichia coli K-12 | CC25 | 0.5000 | 1 | 1 |
| novobiocin | Escherichia coli K-12 | Activity | 3.1000 | 1 | 1 |
| clorobiocin | Escherichia coli K-12 | Activity | 1.6000 | 1 | 1 |
Solid-phase synthesis and biological evaluation of piperazine-based novel bacterial topoisomerase inhibitors.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 57, 2022
Design and synthesis of ciprofloxacin-sulfonamide hybrids to manipulate ciprofloxacin pharmacological qualities: Potency and side effects.European journal of medicinal chemistry, , Jan-15, Volume: 228, 2022
New potent ciprofloxacin-uracil conjugates as DNA gyrase and topoisomerase IV inhibitors against methicillin-resistant Staphylococcus aureus.Bioorganic & medicinal chemistry, , 11-01, Volume: 73, 2022
Discovery and structure-activity relationships of a novel oxazolidinone class of bacterial type II topoisomerase inhibitors.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 65, 2022
[no title available]RSC medicinal chemistry, , Jul-20, Volume: 13, Issue:7, 2022
Design, synthesis and structure-activity relationships of novel 15-membered macrolides: Quinolone/quinoline-containing sidechains tethered to the C-6 position of azithromycin acylides.European journal of medicinal chemistry, , May-01, Volume: 193, 2020
Directing Drugs to Bugs: Antibiotic-Carbohydrate Conjugates Targeting Biofilm-Associated Lectins of Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria.Journal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
Identification of a potent small-molecule inhibitor of bacterial DNA repair that potentiates quinolone antibiotic activity in methicillin-resistant Staphylococcus aureus.Bioorganic & medicinal chemistry, , 10-15, Volume: 27, Issue:20, 2019
Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Virtual Screening Approach and Investigation of Structure-Activity Relationships To Discover Novel Bacterial Topoisomerase Inhibitors Targeting Gram-Positive and Gram-Negative Pathogens.Journal of medicinal chemistry, , 08-22, Volume: 62, Issue:16, 2019
Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-Pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-negative Bacteria.Journal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
Imidazopyrazinones (IPYs): Non-Quinolone Bacterial Topoisomerase Inhibitors Showing Partial Cross-Resistance with Quinolones.Journal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
Targeting quinolone- and aminocoumarin-resistant bacteria with new gyramide analogs that inhibit DNA gyrase.MedChemComm, , Volume: 8, Issue:5, 2017
Search for factors affecting antibacterial activity and toxicity of 1,2,4-triazole-ciprofloxacin hybrids.European journal of medicinal chemistry, , Jun-05, Volume: 97, 2015
Novel 3-arylfuran-2(5H)-one-fluoroquinolone hybrid: design, synthesis and evaluation as antibacterial agent.Bioorganic & medicinal chemistry, , Jul-15, Volume: 22, Issue:14, 2014
Novel DNA gyrase inhibiting spiropyrimidinetriones with a benzisoxazole scaffold: SAR and in vivo characterization.Journal of medicinal chemistry, , Nov-13, Volume: 57, Issue:21, 2014
Synthesis, structure-activity relationship studies, and antibacterial evaluation of 4-chromanones and chalcones, as well as olympicin A and derivatives.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Comparison of in vitro activities of fluoroquinolone-like 2,4- and 1,3-diones.Antimicrobial agents and chemotherapy, , Volume: 54, Issue:7, 2010
DNA gyrase from the albicidin producer Xanthomonas albilineans has multiple-antibiotic-resistance and unusual enzymatic properties.Antimicrobial agents and chemotherapy, , Volume: 52, Issue:4, 2008
Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 16, Issue:5, 2006
Isothiazolopyridones: synthesis, structure, and biological activity of a new class of antibacterial agents.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.Journal of medicinal chemistry, , Nov-02, Volume: 49, Issue:22, 2006
Synthesis and structural-activity relationships of 3-hydroxyquinazoline-2,4-dione antibacterial agents.Bioorganic & medicinal chemistry letters, , Sep-06, Volume: 14, Issue:17, 2004
Structure-activity relationship in the oxazolidinone-quinolone hybrid series: influence of the central spacer on the antibacterial activity and the mode of action.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 13, Issue:23, 2003
Synthesis, structure-activity relationship studies, and antibacterial evaluation of 4-chromanones and chalcones, as well as olympicin A and derivatives.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.Antimicrobial agents and chemotherapy, , Volume: 52, Issue:8, 2008
Design and synthesis of aminothiazolyl norfloxacin analogues as potential antimicrobial agents and their biological evaluation.European journal of medicinal chemistry, , Apr-01, Volume: 167, 2019
Isothiazolopyridones: synthesis, structure, and biological activity of a new class of antibacterial agents.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 16, Issue:5, 2006
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.Journal of medicinal chemistry, , Nov-02, Volume: 49, Issue:22, 2006
Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria.Journal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.Journal of medicinal chemistry, , Nov-02, Volume: 49, Issue:22, 2006
New dual ATP-competitive inhibitors of bacterial DNA gyrase and topoisomerase IV active against ESKAPE pathogens.European journal of medicinal chemistry, , Mar-05, Volume: 213, 2021
Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors.Bioorganic & medicinal chemistry, , 11-15, Volume: 28, Issue:22, 2020
Exploring the Chemical Space of Benzothiazole-Based DNA Gyrase B Inhibitors.ACS medicinal chemistry letters, , Dec-10, Volume: 11, Issue:12, 2020
An optimised series of substituted N-phenylpyrrolamides as DNA gyrase B inhibitors.European journal of medicinal chemistry, , Apr-01, Volume: 167, 2019
New MedChemComm, , Jun-01, Volume: 10, Issue:6, 2019
Targeting quinolone- and aminocoumarin-resistant bacteria with new gyramide analogs that inhibit DNA gyrase.MedChemComm, , Volume: 8, Issue:5, 2017
Discovery of 4,5,6,7-Tetrahydrobenzo[1,2-d]thiazoles as Novel DNA Gyrase Inhibitors Targeting the ATP-Binding Site.Journal of medicinal chemistry, , Jul-23, Volume: 58, Issue:14, 2015
Biological activities of novel gyrase inhibitors of the aminocoumarin class.Antimicrobial agents and chemotherapy, , Volume: 52, Issue:6, 2008
DNA gyrase from the albicidin producer Xanthomonas albilineans has multiple-antibiotic-resistance and unusual enzymatic properties.Antimicrobial agents and chemotherapy, , Volume: 52, Issue:4, 2008
Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationships.Journal of medicinal chemistry, , Sep-11, Volume: 51, Issue:17, 2008