Recent advances in DNA gyrase-targeted antimicrobial agents
Antimicrobial resistance is one of the greatest challenges facing the world today. In the
United States alone, it is responsible for the death of more than 20,000 people each year …
United States alone, it is responsible for the death of more than 20,000 people each year …
Modular and diverse synthesis of amino acids via asymmetric decarboxylative protonation of aminomalonic acids
Stereoselective protonation is a challenge in asymmetric catalysis. The small size and high
rate of transfer of protons mean that face-selective delivery to planar intermediates is hard to …
rate of transfer of protons mean that face-selective delivery to planar intermediates is hard to …
Recent advancements in the medicinal chemistry of bacterial type II topoisomerase inhibitors
Replication proteins are sought as a potential targets for antimicrobial agents. Despite their
promising target characteristics, only topoisomerase II inhibitors targeting DNA gyrase …
promising target characteristics, only topoisomerase II inhibitors targeting DNA gyrase …
Antimicrobial evaluation of thiadiazino and thiazolo quinoxaline hybrids as potential DNA gyrase inhibitors; design, synthesis, characterization and morphological …
YA Ammar, AA Farag, AM Ali, SA Hessein, AA Askar… - Bioorganic …, 2020 - Elsevier
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 …
derivatives was designed and synthetized from the reaction of 2, 3-dichloro-6 …
New dual inhibitors of bacterial topoisomerases with broad-spectrum antibacterial activity and in vivo efficacy against vancomycin-intermediate Staphylococcus …
A new series of dual low nanomolar benzothiazole inhibitors of bacterial DNA gyrase and
topoisomerase IV were developed. The resulting compounds show excellent broad …
topoisomerase IV were developed. The resulting compounds show excellent broad …
Identification of promising anti-DNA gyrase antibacterial compounds using de novo design, molecular docking and molecular dynamics studies
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 …
million deaths result annually from bacterial infections worldwide. Therefore, there is a …
An optimised series of substituted N-phenylpyrrolamides as DNA gyrase B inhibitors
ATP competitive inhibitors of DNA gyrase and topoisomerase IV have great therapeutic
potential, but none of the described synthetic compounds has so far reached the market. To …
potential, but none of the described synthetic compounds has so far reached the market. To …
Supramolecular assemblies mimicking neutrophil extracellular traps for MRSE infection control
Neutrophil extracellular traps (NETs) stick to bacteria and prevent infections in vivo, whose
activation is upon inflammatory stimuli along with the sudden increase of reactive oxygen …
activation is upon inflammatory stimuli along with the sudden increase of reactive oxygen …
New dual ATP-competitive inhibitors of bacterial DNA gyrase and topoisomerase IV active against ESKAPE pathogens
The rise in multidrug-resistant bacteria defines the need for identification of new antibacterial
agents that are less prone to resistance acquisition. Compounds that simultaneously inhibit …
agents that are less prone to resistance acquisition. Compounds that simultaneously inhibit …
Novel 2-arylbenzothiazole DNA gyrase inhibitors: Synthesis, antimicrobial evaluation, QSAR and molecular docking studies
A series of new 2-arylbenzothiazole derivatives (4, 5, 6a-j, 7a-i and 8a, b) was synthesized
and tested for their antimicrobial activity against different Gram-positive, Gram-negative …
and tested for their antimicrobial activity against different Gram-positive, Gram-negative …