89 articles for thisTarget
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Discovery of substituted oxadiazoles as a novel scaffold for DNA gyrase inhibitors.
University of Ljubljana
Quinolone antibacterials: synthesis and biological activity of carbon isosteres of the 1-piperazinyl and 3-amino-1-pyrrolidinyl side chains.
Warner-Lambert
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
Warner-Lambert
Design, synthesis and structure-activity relationship studies of novel indazole analogues as DNA gyrase inhibitors with Gram-positive antibacterial activity.
Dainippon Pharmaceutical
Fine Tuning of physico-chemical parameters to optimise a new series of novobiocin analogues.
Aventis Pharma
DNA gyrase inhibitory activity of ellagic acid derivatives.
R. W. Johnson Pharmaceutical Research Institute
New N-phenyl-4,5-dibromopyrrolamides and N-Phenylindolamides as ATPase inhibitors of DNA gyrase.
University of Ljubljana
Fragment-based discovery of DNA gyrase inhibitors targeting the ATPase subunit of GyrB.
Cubist Pharmaceuticals
The discovery of a novel antibiotic for the treatment of Clostridium difficile infections: a story of an effective academic-industrial partnership.
University College London
Chemical conjugation of 2-hexadecynoic acid to C5-curcumin enhances its antibacterial activity against multi-drug resistant bacteria.
Inter American University of Puerto Rico
Discovery of WQ-3810: Design, synthesis, and evaluation of 7-(3-alkylaminoazetidin-1-yl)fluoro-quinolones as orally active antibacterial agents.
Wakunaga Pharmaceutical
Discovery and Characterization of a Water-Soluble Prodrug of a Dual Inhibitor of Bacterial DNA Gyrase and Topoisomerase IV.
Vertex Pharmaceuticals
Novel DNA gyrase inhibiting spiropyrimidinetriones with a benzisoxazole scaffold: SAR and in vivo characterization.
Astrazeneca
Discovery of 4,5,6,7-Tetrahydrobenzo[1,2-d]thiazoles as Novel DNA Gyrase Inhibitors Targeting the ATP-Binding Site.
University of Ljubljana
Search for factors affecting antibacterial activity and toxicity of 1,2,4-triazole-ciprofloxacin hybrids.
Medical University
Synthesis, structure-activity relationship studies, and antibacterial evaluation of 4-chromanones and chalcones, as well as olympicin A and derivatives.
University of Hawaii At Hilo
Chiral DNA gyrase inhibitors. 3. Probing the chiral preference of the active site of DNA gyrase. Synthesis of 10-fluoro-6-methyl-6,7-dihydro-9-piperazinyl- 2H-benzo[a]quinolizin-20-one-3-carboxylic acid analogues.
University of Kansas
Design, synthesis, and characterization of novel tetrahydropyran-based bacterial topoisomerase inhibitors with potent anti-gram-positive activity.
Actelion Pharmaceuticals
DNA gyrase from the albicidin producer Xanthomonas albilineans has multiple-antibiotic-resistance and unusual enzymatic properties.
The University of Queensland
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
Pfizer
New potent ciprofloxacin-uracil conjugates as DNA gyrase and topoisomerase IV inhibitors against methicillin-resistant Staphylococcus aureus.
Al-Azhar University
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
University of Cape Town
Isothiazolopyridones: synthesis, structure, and biological activity of a new class of antibacterial agents.
Achillion Pharmaceuticals
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.
Achillion Pharmaceuticals
Discovery and structure-activity relationships of a novel oxazolidinone class of bacterial type II topoisomerase inhibitors.
Redx Anti-Infectives
1,3-Dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Expanding Structural Diversity and the Antibacterial Spectrum.
The Ohio State University
Solid-phase synthesis and biological evaluation of piperazine-based novel bacterial topoisomerase inhibitors.
Technical University of Denmark
Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.
Central South University
Research progress in biological activities of isochroman derivatives.
Shaanxi University of Chinese Medicine
design of type II topoisomerase inhibitors as potential antimicrobial agents targeting a novel binding region.
University of Leeds
Design and synthesis of ciprofloxacin-sulfonamide hybrids to manipulate ciprofloxacin pharmacological qualities: Potency and side effects.
Cairo University
Optimization of TopoIV Potency, ADMET Properties, and hERG Inhibition of 5-Amino-1,3-dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Identification of a Lead with
The Ohio State University
Structurally Optimized Potent Dual-Targeting NBTI Antibacterials with an Enhanced Bifurcated Halogen-Bonding Propensity.
National Institute of Chemistry
Structure-activity relationship in the oxazolidinone-quinolone hybrid series: influence of the central spacer on the antibacterial activity and the mode of action.
Morphochem
New dual ATP-competitive inhibitors of bacterial DNA gyrase and topoisomerase IV active against ESKAPE pathogens.
University of Ljubljana
Design, synthesis and bioactivity evaluation of novel pyrazole linked phenylthiazole derivatives in context of antibacterial activity.
Griffith University
Dioxane-Linked Amide Derivatives as Novel Bacterial Topoisomerase Inhibitors against Gram-Positive
The Ohio State University
Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors.
Taisho Pharmaceutical
Rational design, synthesis and testing of novel tricyclic topoisomerase inhibitors for the treatment of bacterial infections part 2.
Redx Anti-Infectives
Design, synthesis and structure-activity relationships of novel 15-membered macrolides: Quinolone/quinoline-containing sidechains tethered to the C-6 position of azithromycin acylides.
Beijing Institute of Technology
One-pot synthesis and molecular docking of some new spiropyranindol-2-one derivatives as immunomodulatory agents and in vitro antimicrobial potential with DNA gyrase inhibitor.
King Khalid University
Directing Drugs to Bugs: Antibiotic-Carbohydrate Conjugates Targeting Biofilm-Associated Lectins of
Helmholtz Institute For Pharmaceutical Research Saarland (Hips)
Exploring the Chemical Space of Benzothiazole-Based DNA Gyrase B Inhibitors.
University of Ljubljana
An optimised series of substituted N-phenylpyrrolamides as DNA gyrase B inhibitors.
University of Ljubljana
Design and synthesis of aminothiazolyl norfloxacin analogues as potential antimicrobial agents and their biological evaluation.
Southwest University
Identification of an ethyl 5,6-dihydropyrazolo[1,5-c]quinazoline-1-carboxylate as a catalytic inhibitor of DNA gyrase.
University of Iowa
Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria.
Novartis Institutes For Biomedical Research
Two Decades of Successful SAR-Grounded Stories of the Novel Bacterial Topoisomerase Inhibitors (NBTIs).
National Institute of Chemistry
New Broad-Spectrum Antibiotics Containing a Pyrrolobenzodiazepine Ring with Activity against Multidrug-Resistant Gram-Negative Bacteria.
King'S College London
Discovery and development of novel rhodanine derivatives targeting enoyl-acyl carrier protein reductase.
Nanjing University
Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
Medical University of Gdansk
Virtual Screening Approach and Investigation of Structure-Activity Relationships To Discover Novel Bacterial Topoisomerase Inhibitors Targeting Gram-Positive and Gram-Negative Pathogens.
Angelini
Switching on the activity of 1,5-diaryl-pyrrole derivatives against drug-resistant ESKAPE bacteria: Structure-activity relationships and mode of action studies.
Sapienza University of Rome
1,2,4-Triazole-quinoline/quinolone hybrids as potential anti-bacterial agents.
Henan University of Chinese Medicine
Structure-guided design of antibacterials that allosterically inhibit DNA gyrase.
Glaxosmithkline
Design, Synthesis, and Biological Evaluation of Novel DNA Gyrase-Inhibiting Spiropyrimidinetriones as Potent Antibiotics for Treatment of Infections Caused by Multidrug-Resistant Gram-Positive Bacteria.
Chinese Academy of Sciences
Second-generation antibacterial benzimidazole ureas: discovery of a preclinical candidate with reduced metabolic liability.
Vertex Pharmaceuticals
Structure-guided design and development of novel benzimidazole class of compounds targeting DNA gyraseB enzyme of Staphylococcus aureus.
Birla Institute of Technology & Science-Pilani
Novel 3-arylfuran-2(5H)-one-fluoroquinolone hybrid: design, synthesis and evaluation as antibacterial agent.
Jishou University
Design, synthesis and biological evaluation of ?-substituted isonipecotic acid benzothiazole analogues as potent bacterial type II topoisomerase inhibitors.
Biota Holdings
Novel quinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV.
Pfizer
Kibdelomycin A, a congener of kibdelomycin, derivatives and their antibacterial activities.
Merck Research Laboratories
Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).
Achillion Pharmaceuticals
Comparison of in vitro activities of fluoroquinolone-like 2,4- and 1,3-diones.
University of Minnesota Medical School
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
Daiichi Sankyo
Synthesis, structure and antibacterial activity of new 2-(1-(2-(substituted-phenyl)-5-methyloxazol-4-yl)-3-(2-substitued-phenyl)-4,5-dihydro-1H-pyrazol-5-yl)-7-substitued-1,2,3,4-tetrahydroisoquinoline derivatives.
Anhui University of Technology
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
Achillion Pharmaceuticals
Synthesis, structure and antibacterial activity of novel 1-(5-substituted-3-substituted-4,5-dihydropyrazol-1-yl)ethanone oxime ester derivatives.
Anhui University of Technology
Synthesis and antibacterial activity of novel pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid derivatives carrying the 3-cyclopropylaminomethyl-4-substituted-1-pyrrolidinyl group as a C-10 substituent.
Kyorin Pharmaceutical
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
Achillion Pharmaceuticals
Synthesis and antibacterial activity of a novel series of DNA gyrase inhibitors: 5-[(E)-2-arylvinyl]pyrazoles.
Dainippon Pharmaceutical
Synthesis and antibacterial activity of a novel series of potent DNA gyrase inhibitors. Pyrazole derivatives.
Dainippon Pharmaceutical
Discovery of (3S)-amino-(4R)-ethylpiperidinyl quinolones as potent antibacterial agents with a broad spectrum of activity and activity against resistant pathogens.
Procter & Gamble Pharmaceuticals
Potent 6-desfluoro-8-methylquinolones as new lead compounds in antibacterial chemotherapy.
Universit£
Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1- pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy.
Warner-Lambert
Synthesis and anti-staphylococcal activity of novel bacterial topoisomerase inhibitors with a 5-amino-1,3-dioxane linker moiety.
The Ohio State University
Imidazopyrazinones (IPYs): Non-Quinolone Bacterial Topoisomerase Inhibitors Showing Partial Cross-Resistance with Quinolones.
Sanofi R&D
Design and synthesis of novel 1H-tetrazol-5-amine based potent antimicrobial agents: DNA topoisomerase IV and gyrase affinity evaluation supported by molecular docking studies.
Medical University of Warsaw
New developments in non-quinolone-based antibiotics for the inhibiton of bacterial gyrase and topoisomerase IV.
Islamia College University
Drug efficacy of novel 3-O-methoxy-4-halo disubstituted 5,7-dimethoxy chromans; evaluated via DNA gyrase inhibition, bacterial cell wall lesion and antibacterial prospective.
Bharathiar University
Design, synthesis, and evaluation of novel N-1 fluoroquinolone derivatives: Probing for binding contact with the active site tyrosine of gyrase.
University of Iowa
Discovery and Optimization of Isoquinoline Ethyl Ureas as Antibacterial Agents.
Actelion Pharmaceuticals
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.
Vertex Pharmaceuticals
Antibacterial activity and mechanism of action of a novel anilinouracil-fluoroquinolone hybrid compound.
Microbiotix