Results 11 to 20 of about 1,477,235 (156)

Discovery of Benzopyrone-Based Candidates as Potential Antimicrobial and Photochemotherapeutic Agents through Inhibition of DNA Gyrase Enzyme B: Design, Synthesis, In Vitro and In Silico Evaluation [PDF]

open access: yesPharmaceuticals
Bacterial DNA gyrase is considered one of the validated targets for antibacterial drug discovery. Benzopyrones have been reported as promising derivatives that inhibit bacterial DNA gyrase B through competitive binding into the ATP binding site of the B ...
Akram Abd El-Haleem   +6 more
doaj   +2 more sources

Experimental and Molecular Docking Studies of Cyclic Diphenyl Phosphonates as DNA Gyrase Inhibitors for Fluoroquinolone-Resistant Pathogens

open access: yesAntibiotics, 2022
DNA gyrase and topoisomerase IV are proven to be validated targets in the design of novel antibacterial drugs. In this study, we report the antibacterial evaluation and molecular docking studies of previously synthesized two series of cyclic ...
Neveen M. Saleh   +7 more
doaj   +1 more source

Towards Conformation-Sensitive Inhibition of Gyrase: Implications of Mechanistic Insight for the Identification and Improvement of Inhibitors

open access: yesMolecules, 2021
Gyrase is a bacterial type IIA topoisomerase that catalyzes negative supercoiling of DNA. The enzyme is essential in bacteria and is a validated drug target in the treatment of bacterial infections.
Dagmar Klostermeier
doaj   +1 more source

RNA INTERFERNCE (RNAI) FOR SOME GENES FROM BABESIA BOVIS [PDF]

open access: yesResearch Journal of Applied Biotechnology, 2016
Babesia parasites are responsible for enormous economic losses to the livestock industry worldwide. There is no vaccine available to protect from the infection.
Ikuo Igarashi   +2 more
doaj   +1 more source

Antibacterial small molecules targeting the conserved TOPRIM domain of DNA gyrase. [PDF]

open access: yesPLoS ONE, 2017
To combat the threat of antibiotic-resistant Gram-negative bacteria, novel agents that circumvent established resistance mechanisms are urgently needed.
Scott S Walker   +20 more
doaj   +1 more source

Protein gates in DNA gyrase

open access: yes, 1999
DNA gyrase is a molecular machine comprising a series of protein gates. The opening and closing of these gates enables the passage of one segment of double-stranded DNA (the T segment) through a transient break in another (the G segment). We have blocked
Nicola Louise. Williams (7638380)
core   +6 more sources

Synthesis, structure and antibacterial activity of potent DNA gyrase inhibitors: N'-benzoyl-3-(4-bromophenyl)-1H-pyrazole-5-carbohydrazide derivatives. [PDF]

open access: yesPLoS ONE, 2013
A total of 19 novel (3a-3s) N'-benzoyl-3-(4-bromophenyl)-1H-pyrazole-5-carbohydrazide analogs were designed, synthesized, and evaluated for biological activities as potential DNA gyrase inhibitors. The results showed that compound 3k can strongly inhibit
Juan Sun   +5 more
doaj   +1 more source

Structure based in silico analysis of quinolone resistance in clinical isolates of Salmonella Typhi from India. [PDF]

open access: yesPLoS ONE, 2015
Enteric fever is a major cause of morbidity in several parts of the Indian subcontinent. The treatment for typhoid fever majorly includes the fluoroquinolone group of antibiotics.
Manoj Kumar   +6 more
doaj   +1 more source

The bacteriophage LUZ24 “Igy” peptide inhibits the Pseudomonas DNA gyrase

open access: yesCell Reports, 2021
Summary: The bacterial DNA gyrase complex (GyrA/GyrB) plays a crucial role during DNA replication and serves as a target for multiple antibiotics, including the fluoroquinolones.
Jeroen De Smet   +9 more
doaj   +1 more source

Potent DNA gyrase inhibitors bind asymmetrically to their target using symmetrical bifurcated halogen bonds

open access: yesNature Communications, 2021
The mechanism of DNA gyrase inhibitor stabilization of single-strand DNA cleavage breaks by DNA gyrase has been hypothetical. Here, the authors show experimental evidence of the mechanism using a library of inhibitors with improved binding and employ ...
Anja Kolarič   +9 more
doaj   +1 more source

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