Design, synthesis, molecular modeling, and antimicrobial potential of novel 3-[(1H-pyrazol-3-yl)imino]indolin-2-one derivatives as DNA gyrase inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202100266
Abstract: A series of 3-[(1H-pyrazol-3-yl)imino]indolin-2-one derivatives were designed using the molecular hybridization method, characterized using different spectroscopic techniques, and evaluated for their in vitro antimicrobial activity. Most of the target compounds demonstrated good to moderate antimicrobial… read more here.
Keywords: one derivatives; pyrazol imino; dna gyrase; indolin one ... See more keywords
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
New pyrrole derivatives as DNA gyrase and 14α-demethylase inhibitors: Design, synthesis, antimicrobial evaluation, and molecular docking.
Sign Up to like & getrecommendations! Published in 2023 at "Drug development research"
DOI: 10.1002/ddr.22080
Abstract: An efficient one-pot reaction utilizing readily available chemical reagents was used to prepare novel 2-amino-1,5-diaryl-1H-pyrrole-3-carbonitrile derivatives and the structures of these compounds were validated by spectroscopic data and elemental analyses. All the synthetic compounds were… read more here.
Keywords: demethylase; dna gyrase; ic50; gyrase demethylase ... See more keywords
Pharmacophore modeling and molecular dynamics approach to identify putative DNA Gyrase B inhibitors for resistant tuberculosis
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Cellular Biochemistry"
DOI: 10.1002/jcb.27579
Abstract: One of the major mechanisms followed by the therapeutic agents to target the causative organism of TB, mycobacterium tuberculosis (Mtb), involves disruption of the replication cycle of the pathogen DNA. The process involves two steps… read more here.
Keywords: gyrb domain; pharmacophore; domain; dna gyrase ... See more keywords
Novel antimicrobial ciprofloxacin-pyridinium quaternary ammonium salts with improved physicochemical properties and DNA gyrase inhibitory activity
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DOI: 10.1007/s00044-021-02798-3
Abstract: New ciprofloxacin/ quaternary ammonium salts 3a–e were designed and synthesized as potential antimicrobial agents. Most of the prepared derivatives showed promising dual antibacterial/antifungal activities. Compound 3e was the most potent and afforded vast spectrum antibacterial… read more here.
Keywords: ammonium salts; dna gyrase; ciprofloxacin; quaternary ammonium ... 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, green one-pot synthesis and molecular docking study of novel N,N-bis(cyanoacetyl)hydrazines and bis-coumarins as effective inhibitors of DNA gyrase and topoisomerase IV.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.103672
Abstract: A novel, quick, environmentally safe, and one-pot synthesis of a series of N,N-bis(cyanoacetyl)hydrazine derivatives, bis-imino-2H-chromenes and bis-2-oxo-2H-chromene derivatives have been designed. Some selected newly synthesized compounds were investigated in vitro for their antibacterial activity. Compound… read more here.
Keywords: gyrase topoisomerase; dna gyrase; compound; one pot ... See more keywords
Antimicrobial evaluation of thiadiazino and thiazolo quinoxaline hybrids as potential DNA gyrase inhibitors; design, synthesis, characterization and morphological studies.
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DOI: 10.1016/j.bioorg.2020.103841
Abstract: A series of thiadiazino[5,6-b]quinoxaline and thiazolo[4,5-b]quinoxaline derivatives was designed and synthetized from the reaction of 2,3-dichloro-6-(morpholinosulfonyl)quinoxaline (2) with thiosemicarbazide or thiocarbohydrazide and thiourea derivatives to give nineteen quinoxaline derivatives 3-16. All the synthesized compounds were… read more here.
Keywords: quinoxaline; thiazolo quinoxaline; dna gyrase; morphological studies ... See more keywords
Employing bacteria machinery for antibiotic detection: Using DNA gyrase for ciprofloxacin detection
Sign Up to like & getrecommendations! Published in 2021 at "Chemical Engineering Journal"
DOI: 10.1016/j.cej.2020.128135
Abstract: Abstract This work describes a new successful approach for designing biosensors that detect antibiotics. It makes use of a biomimetic strategy, by employing the biochemical target of a given antibiotic as its biorecognition element. This… read more here.
Keywords: detection; response; machinery; antibiotic detection ... See more keywords
Discovery of a Novel DNA Gyrase-Targeting Antibiotic through the Chemical Perturbation of Streptomyces venezuelae Sporulation
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DOI: 10.1016/j.chembiol.2019.06.002
Abstract: Summary Common approaches to antibiotic discovery include small-molecule screens for growth inhibition in target pathogens and screens for inhibitors of purified enzymes. These approaches have a shared intent of seeking to directly target a vital… read more here.
Keywords: sporulation; discovery; streptomyces venezuelae; dna gyrase ... See more keywords
DNA topoisomerase I and DNA gyrase as targets for TB therapy.
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DOI: 10.1016/j.drudis.2016.11.006
Abstract: Tuberculosis (TB) is the deadliest bacterial disease in the world. New therapeutic agents are urgently needed to replace existing drugs for which resistance is a significant problem. DNA topoisomerases are well-validated targets for antimicrobial and… read more here.
Keywords: dna topoisomerase; topoisomerase dna; dna gyrase; dna ... See more keywords