New 1,2,4-oxadiazole/pyrrolidine hybrids as topoisomerase IV and DNA gyrase inhibitors with promising antibacterial activity.
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202100516
Abstract: A series of hybridized pyrrolidine compounds with a 1,2,4-oxadiazole moiety were synthesized to develop effective molecules against the enzymes DNA gyrase and topoisomerase IV (Topo IV). Compounds 8-20 were developed based on a previously disclosed… read more here.
Keywords: new oxadiazole; gyrase; activity; topoisomerase ... See more keywords
Role of unique loops in oligomerization and ATPase function of Plasmodium falciparum gyrase B
Sign Up to like & getrecommendations! Published in 2021 at "Protein Science"
DOI: 10.1002/pro.4217
Abstract: DNA gyrase is an ATP dependent Type IIA topoisomerase that is unique to prokaryotes. Interestingly DNA gyrase has also been found in the apicoplasts of apicomplexan parasites like Plasmodium falciparum (Pf) the causative agent of… read more here.
Keywords: pfgyrbn; gyrase; region; atpase ... See more keywords
Molecular characterization of pea DNA gyrase-A reveals dual localization of protein in plastid and mitochondria
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Plant Biochemistry and Biotechnology"
DOI: 10.1007/s13562-018-0478-2
Abstract: Gyrases are a class of Topoisomerase II that facilitate ATP dependent negative supercoiling of DNA during transcription and replication. They aid in strand breakage during chromosome condensation and take part in separation of intertwined DNA… read more here.
Keywords: molecular characterization; pea dna; dna; gyrase ... See more keywords
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.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b01750
Abstract: Spiropyrimidinetriones are a novel class of antibacterial agents that target the bacterial type II topoisomerase via a new mode of action. Compound ETX0914 is thus far the only drug from this class that is being… read more here.
Keywords: gram positive; design synthesis; biological evaluation; gyrase ... See more keywords
A Series of Spiropyrimidinetriones that Enhances DNA Cleavage Mediated by Mycobacterium tuberculosis Gyrase
Sign Up to like & getrecommendations! Published in 2023 at "ACS Infectious Diseases"
DOI: 10.1021/acsinfecdis.3c00012
Abstract: The rise in drug-resistant tuberculosis has necessitated the search for alternative antibacterial treatments. Spiropyrimidinetriones (SPTs) represent an important new class of compounds that work through gyrase, the cytotoxic target of fluoroquinolone antibacterials. The present study… read more here.
Keywords: mycobacterium tuberculosis; dna cleavage; tuberculosis; series ... See more keywords
Discovery of Novel Inhibitors of Bacterial DNA Gyrase Using a QSAR-Based Approach
Sign Up to like & getrecommendations! Published in 2022 at "ACS Omega"
DOI: 10.1021/acsomega.2c04310
Abstract: Type II topoisomerases like DNA gyrase initiate ATP-dependent negative supercoils in bacterial DNA. It is critical in all of the bacteria but is missing from eukaryotes, making it a striking target for antibacterials. Ciprofloxacin is… read more here.
Keywords: bacterial dna; dna gyrase; gyrase; qsar model ... See more keywords
Microwave-assisted synthesis and in vitro and in silico studies of pyrano[3,2-c]quinoline-3-carboxylates as dual acting anti-cancer and anti-microbial agents and potential topoisomerase II and DNA-gyrase inhibitors
Sign Up to like & getrecommendations! Published in 2025 at "RSC Advances"
DOI: 10.1039/d4ra06201a
Abstract: A microwave-assisted method was utilized to synthesize novel pyranoquinolone derivatives as dual acting topoisomerase II/DNA gyrase inhibitors with apoptosis induction ability for halting lung cancer and staphylococcal infection. Herein, the designed rationale was directed toward… read more here.
Keywords: topoisomerase dna; gyrase; dna gyrase; gyrase inhibitors ... See more keywords
Identification of new DNA gyrase inhibitors based on bioactive compounds from streptomyces: structure-based virtual screening and molecular dynamics simulations approaches
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Biomolecular Structure and Dynamics"
DOI: 10.1080/07391102.2019.1588784
Abstract: Abstract DNA gyrase enzyme has vital role in bacterial survival and can be considered as a potential drug target. Owing to the appearance of resistance to gyrase-targeted drugs, especially fluoroquinolone, screening new compounds which bind… read more here.
Keywords: based virtual; dna; gyrase; dna gyrase ... See more keywords
Identification of promising anti-DNA gyrase antibacterial compounds using de novo design, molecular docking and molecular dynamics studies
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Biomolecular Structure and Dynamics"
DOI: 10.1080/07391102.2019.1617785
Abstract: Abstract The rapidly increasing rate of antibiotic resistance is of great concern. Approximately two million deaths result annually from bacterial infections worldwide. Therefore, there is a paramount requirement to develop innovative and novel antibacterial agents… read more here.
Keywords: gyrase; novo design; dna gyrase; molecular dynamics ... See more keywords
Molecular dynamics simulation guided analysis of the interaction between delafloxacin and Staphylococcus aureus gyrase mutants
Sign Up to like & getrecommendations! Published in 2024 at "Molecular Simulation"
DOI: 10.1080/08927022.2024.2332453
Abstract: ABSTRACT Staphylococcus aureus is a highly virulent nosocomial pathogen producing a wide array of virulence factors to orchestrate a deadly disease. Delafloxacin is a fluoroquinolone antibiotic targeting gyrase to confer its antibacterial properties by stabilising… read more here.
Keywords: gyrase; delafloxacin; simulation; molecular dynamics ... See more keywords
Targeting novel sites in DNA gyrase for development of anti-microbials.
Sign Up to like & getrecommendations! Published in 2022 at "Briefings in functional genomics"
DOI: 10.1093/bfgp/elac029
Abstract: Antimicrobial resistance in bacteria poses major challenges in selection of the therapeutic regime for managing the infectious disease. There is currently an upsurge in the appearance of multiple drug resistance in bacterial pathogens and a… read more here.
Keywords: dna gyrase; novel sites; development; resistance ... See more keywords