Synthesis of a Tetrahydronaphthyridine Spiropyrimidinetrione DNA Gyrase Inhibiting Antibacterial Agent - Differential Substitution at all Five Carbon Atoms of Pyridine.

2014 ◽  
Vol 16 (24) ◽  
pp. 6456-6459 ◽  
Author(s):  
Gregory S. Basarab ◽  
Vincent Galullo ◽  
Nancy DeGrace ◽  
Sheila Hauck ◽  
Camil Joubran ◽  
...  
Keyword(s):  
Antibacterial Agent ◽  
Dna Gyrase ◽  
Differential Substitution

Prediction Mechanism of Nevadensin as Antibacterial Agent against S. sanguinis: In vitro and In silico Studies

2021 ◽  
Vol 24 ◽  
Author(s):  
Aldina Amalia Nur Shadrina ◽  
Yetty Herdiyati ◽  
Ika Wiani ◽  
Mieke Hemiawati Satari ◽  
Dikdik Kurnia
Keyword(s):  
Antibacterial Activity ◽  
Molecular Docking ◽  
Dental Caries ◽  
Binding Affinity ◽  
In Silico ◽  
Antibacterial Agent ◽  
In Silico Analysis ◽  
Dna Gyrase ◽  
Silico Analysis

Background: Streptococcus sanguinis can contribute to tooth demineralization, which can lead to dental caries. Antibiotics used indefinitely to treat dental caries can lead to bacterial resistance. Discovering new antibacterial agents from natural products like Ocimum basilicum will help combat antibiotic resistance. In silico analysis (molecular docking) can help determine the lead compound by studying the molecular interaction between the drug and the target receptor (MurA enzyme and DNA gyrase). It is a potential candidate for antibacterial drug development. Objective: The research objective is to isolate the secondary metabolite of O. basilicum extract that has activity against S. sanguinis through in vitro and in silico analysis. Methods: n-Hexane extract of O. basilicum was purified by combining column chromatography with bioactivity-guided. The in vitro antibacterial activity against S. sanguinis was determined using the disc diffusion and microdilution method, while molecular docking simulation of nevadensin (1) with MurA enzyme and DNA gyrase was performed used PyRx 0.8 program. Results: Nevadensin from O. basilicum was successfully isolated and characterized by spectroscopic methods. This compound showed antibacterial activity against S. sanguinis with MIC and MBC values of 3750 and 15000 μg/mL, respectively. In silico analysis showed that the binding affinity to MurA was -8.5 Kcal/mol, and the binding affinity to DNA gyrase was -6.7 Kcal/mol. The binding of nevadensin-MurA is greater than fosfomycin-MurA. Otherwise, Nevadensin-DNA gyrase has a weaker binding affinity than fluoroquinolone-DNA gyrase and chlorhexidine-DNA gyrase. Conclusion: Nevadensin showed potential as a new natural antibacterial agent by inhibiting the MurA enzyme rather than DNA gyrase.

Novel Benzotriazole acetamide derivatives as Benzo-Fused Five-Membered Nitrogen-Containing Heterocycle- Insilico Screening, Molecular Docking, and Synthesis

2021 ◽  
Vol 18 ◽  
Author(s):  
Patil Tejaswini D. ◽  
Amrutkar Sunil V.
Keyword(s):  
Staphylococcus Aureus ◽  
Molecular Docking ◽  
Active Site ◽  
Antibacterial Agent ◽  
Antibacterial Properties ◽  
Dna Gyrase ◽  
Antibacterial Drug ◽  
E Coli ◽  
Fast Development ◽  
Subunit B

Background: DNA gyrase subunit B (1KZN) is an attractive target for antibacterial drug development because of its role in DNA replication. The fast development of antimicrobial medication resistance necessitates the quick discovery of new antimicrobial medicines. Objective: The goal of this research is to design, synthesize, and discover benzo-fused five-membered nitrogen-containing heterocycles that bind to DNA gyrase subunit B via molecular docking (1KZN). Methods: Based on literature research, 2-(1H-1,2,3-Benzotriazol-1-yl)-N-substituted acetamide was synthesized using an efficient method. All synthesized compounds were evaluated for antibacterial activity against three distinct organisms: E. coli, Pseudomonas aeruginosa, Staphylococcus aureus. In a docking investigation, the chemical interacts with the active site of DNA gyrase subunit B (1KZN), indicating that it might have antibacterial action. Conclusion: According to the findings of this research, the compounds 3d and 3f show antibacterial properties. For Staphylococcus aureus, 3c has the potential to be an antibacterial agent.

Haloemodin as Novel Antibacterial Agent Inhibiting DNA Gyrase and Bacterial Topoisomerase I

2014 ◽  
Vol 57 (9) ◽  
pp. 3707-3714 ◽  
Author(s):  
Feixia Duan ◽  
Xiaohong Li ◽  
Suping Cai ◽  
Guang Xin ◽  
Yanyan Wang ◽  
...  
Keyword(s):  
Antibacterial Agent ◽  
Topoisomerase I ◽  
Dna Gyrase

Reverse torque values of abutment screws after dynamic loading: The effects of sealant agents and the taper of conical connections

2020 ◽  
Author(s):  
Arda Ozdiler ◽  
suleyman dayan ◽  
Burc Gencel ◽  
Gulbahar Isık-Ozkol
Keyword(s):  
Dynamic Loading ◽  
Antibacterial Agent ◽  
In Vitro Study ◽  
Control Group ◽  
Silicone Sealant ◽  
Reverse Torque ◽  
The Stability ◽  
Torque Values ◽  
Chlorhexidine Gel

This in vitro study evaluated the influence of taper angles on the internal conical connections of implant systems and of the application of chlorhexidine gel as an antibacterial agent or a polyvinyl siloxane (PVS) sealant on the reverse torque values of abutment screws after dynamic loading. The current study tested four implant systems with different taper angles (5.4°, 12°, 45°, and 60°). Specimens were divided into three groups: control (neither chlorhexidine gel filled nor silicone sealed), 2% chlorhexidine gel-filled or silicone-sealed group, and group subjected to a dynamic load of 50 N at 1 Hz for 500,000 cycles prior to reverse torque measurements. Quantitative positive correlation was observed between the taper angle degree and the percentage of tightening torque loss. However, this correlation was significant only for the 60° connection groups except in the group in which a sealant was applied ( p = 0.013 for the control group, p = 0.007 for the chlorhexidine group). Percentages of decrease in the torque values of the specimens with silicone sealant application were significantly higher compared with both the control and chlorhexidine groups ( p = 0.001, p = 0.002, p = 0.001, and p = 0.002, respectively, according to the increasing taper angles); the percentage of decrease in torque values due to chlorhexidine application was statistically insignificant when compared with the control group. The application of gel-form chlorhexidine as an antibacterial agent does not significantly affect the stability of the implant–abutment connection under dynamic loads. PVS sealants may cause screw loosening under functional loads.

Antibacterial Activity of Thujaoccidentalis,ThujaorientalisandChamaecyparisobtusa

2017 ◽  
Vol 8 (03) ◽  
Author(s):  
Kyoung- Sun Seo ◽  
Seong Woo Jin ◽  
Seongkyu Choi ◽  
Kyeong Won Yun
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Antibacterial Agent ◽  
Methanol Extract ◽  
The Other ◽  
Diffusion Method ◽  
E Coli ◽  
Agar Diffusion ◽  
Agar Diffusion Method ◽  
Crude Methanol Extract

The antibacterial activity of three Cupressaceae plants (Thujaoccidentalis,ThujaorientalisandChamaecyparisobtusa) was tested against three bacteria using the agar diffusion method. The ether and ethylacetate fraction of crude methanol extract from the three plants showed potent antibacterial activity against the tested microorganisms. The result showed that Staphylococcus aureus revealed the most sensitivity among the tested bacteria. Thujaoccidentalisether fraction and Thujaorientalis hexane fraction exhibited the highest antibacterial activity against Staphylococcus aureus. E. coli was shown the highest MIC values compared to the other two tested bacteria, which indicates the lowest antibacterial activity against the bacterium. This study promises an interesting future for designing a potentially active antibacterial agent from the three Cupressaceae plants.

Antibacterial Activities of Sirih Merah (Piper crocatum) Leaf Extracts

2019 ◽  
Vol 5 (3) ◽  
pp. 1-10
Author(s):  
Puspa Julistia Puspita ◽  
Mega Safithri ◽  
Nirmala Peni Sugiharti
Keyword(s):  
Escherichia Coli ◽  
Pseudomonas Aeruginosa ◽  
Antibacterial Agent ◽  
Leaf Extract ◽  
Antibacterial Activities ◽  
Leaf Extracts ◽  
Herbal Plants

Piper crocatum is one of medicinal herbal plants with a large number of benefits. Usually herbal plants have activity as antibacterial agent. Therefore, the objectives of this research were to obtain information on antibacterial activities of the leaf extracts of Piper crocatum againts four types of bacteria, in that Staphylococcus, Bacillus substilis, Escherichia coli, and Pseudomonas aeruginosa and then to analyze the phytochemistry of the leaf extracts of Piper crocatum. The leaves of Piper crocatum were extracted by maceration and reflux using ethanol 30%. The assays of the antibacterial activities and phytochemistry on the extracts were carried out using the method of Maria Bintang. Results showed that the yield of the extraction using ethanol by maceration method was 20.8%. Meanwhile, using the reflux method, the yield was obtained about 26.25%. The phytochemistry analysis showed that the leaf extracts of Piper crocatum contained alkaloid, steroid and tanin. According to this study, it was found that the leaf extract of Piper crocatum can be used to inhibit the growth of B. subtilis and P. aeuruginosa, but can not inhibit the growth of E.coli and S. aureus.

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