DNA Gyrase Is Involved in Chloroplast Nucleoid Partitioning

Background: Thiosemicarbazone, 1,2,3-triazole and their derivatives received great pharmaceutical importance due to their prominent biological activities. In the present study, the molecular hybrid thiosemicarbazone-1,2,3-triazoles derivatives were synthesized and screened for their antimicrobial activities. Methods: A series of thiosemicarbazone clubbed with 1,2,3-triazole derivatives were synthesized via click chemistry approach in good yields. The structures of synthesized compounds were assigned by their spectral data. The in vitro antimicrobial activity was performed by the agar well diffusion method. A molecular docking study was performed to identify the possible mode of action of synthesized derivatives. Results: The compounds 5d, 5h, 5i and 5k have exhibited excellent antimicrobial activities against both antibacterial and antifungal pathogens. The active thiosemicarbazone-1,2,3-triazole derivatives have shown excellent binding affinity towards DNA gyrase. Conclusion: The molecular hybrid thiosemicarbazone-1,2,3-triazole derivatives were synthesized. The newly synthesized compounds were evaluated for their antimicrobial activities. Few of the thiosemicarbazone-1,2,3-triazoles derivatives have exhibited good antimicrobial activities. They have been shown excellent binding affinity towards DNA gyrase.

Docking and 3D QSAR Studies on Substituted Cyclobutylphenyl Quinoline Derivatives as Inhibitors of Bacterial DNA Gyrase

Current Computer - Aided Drug Design ◽

10.2174/1573409914666180516114700 ◽

2018 ◽

Vol 14 (4) ◽

pp. 322-337

Author(s):

Rucha R. Wani ◽

Hemchandra K. Chaudhari

Keyword(s):

Dna Gyrase ◽

3D Qsar ◽

Quinoline Derivatives ◽

Bacterial Dna ◽

Qsar Studies

Quantitative structure-activity relationship model, molecular docking simulation and computational design of some novel compounds against DNA gyrase receptor.

Current Computer - Aided Drug Design ◽

10.2174/1573409916666200625142447 ◽

2020 ◽

Vol 16 ◽

Author(s):

Shola Elijah Adeniji

Keyword(s):

Biological Activity ◽

Molecular Docking ◽

Binding Energy ◽

Biological Activities ◽

Docking Simulation ◽

Dna Gyrase ◽

Computational Design ◽

Multi Drug Resistance ◽

Drug Candidate ◽

Standard Drug

Introduction: Mycobacterium tuberculosis has instigated a serious challenge toward the effective treatment of tuberculosis. The reoccurrence of the resistant strains of the disease to accessible drugs/medications has mandate for the development of more effective anti-tubercular agents with efficient activities. Time expended and costs in discovering and synthesizing new hypothetical drugs with improved biological activity have been a major challenge toward the treatment of multi-drug resistance strain M. tuberculosis (TB). Meanwhile, to solve the problem stated, a new approach i.e. QSAR which establish connection between novel drugs with a better biological against M. tuberculosis is adopted. Methods: The anti-tubercular model established in this study to forecast the biological activities of some anti-tubercular compounds selected and to design new hypothetical drugs is subjective to the molecular descriptors; MATS7s, SM1_DzZ, SpMin4_Bhv, TDB3v and RDF70v. Ligand-receptor interactions between quinoline derivatives and the receptor (DNA gyrase) was carried out using molecular docking technique by employing the PyRx virtual screening software and discovery studio visualizer software. Furthermore, docking study indicates that compounds 20 of the derivatives with promising biological activity have the utmost binding energy of -17.79 kcal/mol. Results: Meanwhile, the interaction of the standard drug; isoniazid with the target enzyme was observed with the binding energy -14.6 kcal/mol which was significantly lesser than the binding energy of the ligand (compound 20).Therefore, compound 20 served as a template structure to designed compounds with more efficient activities. Among the compounds designed; compounds 20p was observed with better anti-tubercular activities with more prominent binding affinities of -24.3kcal/mol. Conclusion: The presumption of this research aid the medicinal chemists and pharmacist to design and synthesis a novel drug candidate against the tuberculosis. Moreover, in-vitro and in-vivo test could be carried out to validate the computational results.

Involvement of DNA gyrase in bacteriophage T7 growth.

Journal of Virology ◽

10.1128/jvi.53.1.296-298.1985 ◽

1985 ◽

Vol 53 (1) ◽

pp. 296-298 ◽

Cited By ~ 4

Author(s):

T R Steck ◽

K Drlica

Keyword(s):

Dna Gyrase ◽

Bacteriophage T7

In Vitro Characterization of the Antibacterial Spectrum of Novel Bacterial Type II Topoisomerase Inhibitors of the Aminobenzimidazole Class

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.50.4.1228-1237.2006 ◽

2006 ◽

Vol 50 (4) ◽

pp. 1228-1237 ◽

Cited By ~ 56

Author(s):

Nagraj Mani ◽

Christian H. Gross ◽

Jonathan D. Parsons ◽

Brian Hanzelka ◽

Ute Müh ◽

...

Keyword(s):

Bacterial Resistance ◽

Wide Spectrum ◽

Dna Gyrase ◽

Antibacterial Activities ◽

Mechanisms Of Action ◽

Fluoroquinolone Resistance ◽

Topoisomerase Iv ◽

Low Frequencies

ABSTRACT Antibiotics with novel mechanisms of action are becoming increasingly important in the battle against bacterial resistance to all currently used classes of antibiotics. Bacterial DNA gyrase and topoisomerase IV (topoIV) are the familiar targets of fluoroquinolone and coumarin antibiotics. Here we present the characterization of two members of a new class of synthetic bacterial topoII ATPase inhibitors: VRT-125853 and VRT-752586. These aminobenzimidazole compounds were potent inhibitors of both DNA gyrase and topoIV and had excellent antibacterial activities against a wide spectrum of problematic pathogens responsible for both nosocomial and community-acquired infections, including staphylococci, streptococci, enterococci, and mycobacteria. Consistent with the novelty of their structures and mechanisms of action, antibacterial potency was unaffected by commonly encountered resistance phenotypes, including fluoroquinolone resistance. In time-kill assays, VRT-125853 and VRT-752586 were bactericidal against Staphylococcus aureus, Streptococcus pneumoniae, Enterococcus faecalis, and Haemophilus influenzae, causing 3-log reductions in viable cells within 24 h. Finally, similar to the fluoroquinolones, relatively low frequencies of spontaneous resistance to VRT-125853 and VRT-752586 were found, a property consistent with their in vitro dual-targeting activities.

New 1,4-dihydro[1,8]naphthyridine derivatives as DNA gyrase inhibitors

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2017.01.073 ◽

2017 ◽

Vol 27 (5) ◽

pp. 1162-1168 ◽

Cited By ~ 13

Author(s):

Hülya Karaca Gençer ◽

Serkan Levent ◽

Ulviye Acar Çevik ◽

Yusuf Özkay ◽

Sinem Ilgın

Keyword(s):

Dna Gyrase ◽

Gyrase Inhibitors

The intrinsic ATPase of DNA gyrase.

Journal of Biological Chemistry ◽

10.1016/s0021-9258(18)43737-4 ◽

1980 ◽

Vol 255 (13) ◽

pp. 6299-6306 ◽

Cited By ~ 6

Author(s):

A. Sugino ◽

N.R. Cozzarelli

Keyword(s):

Dna Gyrase