scholarly journals Non-natural 2H-azirine-2-carboxylic acids: an expedient synthesis and antimicrobial activity

RSC Advances ◽  
2019 ◽  
Vol 9 (65) ◽  
pp. 37901-37905 ◽  
Author(s):  
Pavel A. Sakharov ◽  
Alexander N. Koronatov ◽  
Alexander F. Khlebnikov ◽  
Mikhail S. Novikov ◽  
Artem G. Glukharev ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Carboxylic Acids ◽  
High Antibacterial Activity ◽  
Low Cytotoxicity ◽  
Eskape Pathogens

A method for the synthesis of 2H-azirine-2-carboxylic acids with high antibacterial activity against ESKAPE pathogens and low cytotoxicity was developed.

Benzannulated Re(i)–NHC complexes: synthesis, photophysical properties and antimicrobial activity

2017 ◽  
Vol 46 (44) ◽  
pp. 15269-15279 ◽  
Author(s):  
Daniel Siegmund ◽  
Nicole Lorenz ◽  
Yvonne Gothe ◽  
Christian Spies ◽  
Bastian Geissler ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Photophysical Properties ◽  
High Antibacterial Activity ◽  
Strong Luminescence

A series of novel Re(i)(CO)3–NHC complexes bearing unsubstituted benzimidazol-2-ylidene ligands is presented which provide strong luminescence as well as high antibacterial activity.

scholarly journals Evaluation of Samarium Doped Hydroxyapatite, Ceramics for Medical Application: Antimicrobial Activity

2015 ◽  
Vol 2015 ◽  
pp. 1-11 ◽  
Author(s):  
C. S. Ciobanu ◽  
S. L. Iconaru ◽  
C. L. Popa ◽  
M. Motelica-Heino ◽  
D. Predoi
Keyword(s):  
Electron Microscopy ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Enterococcus Faecalis ◽  
Medical Application ◽  
Inhibitory Effect ◽  
Linear Increase ◽  
High Antibacterial Activity ◽  
Hydroxyapatite Ceramics ◽  
Transmission Electron

Samarium doped hydroxyapatite (Sm:HAp),Ca10-xSmx(PO4)6(OH)2(HAp), bionanoparticles with differentxSmhave been successfully synthesized by coprecipitation method. Detailed characterization of samarium doped hydroxyapatite nanoparticles (Sm:HAp-NPs) was carried out using X-ray diffraction (XRD), scanning electron microscopy (SEM), transmission electron microscopy (TEM), and Fourier transform infrared spectroscopy (FTIR). The biocompatibility of samarium doped hydroxyapatite was assessed by cell viability. The antibacterial activity of the Sm:HAp-NPs was tested against Gram-negative bacteria (Pseudomonas aeruginosaandEscherichia coli) and Gram-positive bacteria (Enterococcus faecalisandStaphylococcus aureus). A linear increase of antimicrobial activity ofP. aeruginosahas been observed when concentrations of Sm:HAp-NPs in the samples withxSm=0.02were higher than 0.125 mg/mL. For Sm:HAp-NPs withxSm=0.05a significant increase of antibacterial activity onE. coliwas observed in the range 0.5–1 mg/mL. For low concentrations of Sm:HAp-NPs (xSm=0.05) from 0.031 to 0.125 mg/mL a high antibacterial activity onEnterococcus faecalishas been noticed. A growth of the inhibitory effect onS. aureuswas observed for all concentrations of Sm:HAp-NPs withxSm=0.02.

Synthesis of some 1-aryl-1,4-dihydro-4-oxoquinoline-3-carboxylic acids and their antibacterial activity

1989 ◽  
Vol 54 (8) ◽  
pp. 2181-2189 ◽  
Author(s):  
Stanislav Rádl ◽  
Viktor Zikán
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Carboxylic Acids ◽  
Hydrogen Fluoride ◽  
Ferrous Sulfate ◽  
Ethyl Esters ◽  
Direct Arylation

1,4-Dihydro-4-oxoquinoline-3-carboxylic acids VIIIc and VIIId were prepared via their ethyl esters VIIIa and VIIIb, which were obtained by a direct arylation of ethyl 7-chloro-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylate (VIa). When treated with piperazine or N-methylpiperazine compound VIIId yields VIIIe or VIIIf, respectively. Reduction of VIIId, VIIIe, and VIIIf with ferrous sulfate yields VIIIg, VIIIh, and VIIIi, respectively. Diazotization and introduction of fluorine into VIIIg using hydrogen fluoride-pyridine yields VIIIj. The compounds prepared were tested for their antimicrobial activity in vitro.

scholarly journals Antimicrobial activity of mouth rinses against bacteria that initially colonizes dental’s surface

2019 ◽  
Vol 48 ◽  
Author(s):  
Isaac Jordão de Souza ARAÚJO ◽  
Marília Souza de CARVALHO ◽  
Thaís Rossini de OLIVEIRA ◽  
Regina Maria PUPPIN-RONTANI ◽  
José Francisco HÖFLING ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Bacterial Species ◽  
Cetylpyridinium Chloride ◽  
Dental Biofilm ◽  
High Antibacterial Activity ◽  
Mouth Rinses ◽  
Post Hoc ◽  
Antimicrobial Effectiveness

Abstract Introduction Much advertising in mouthwash is conveyed in all media appealing to the anti-plaque effect and rendering a disservice to the community. Mouth rinses are available over-the-count and differ on their compositions and antimicrobial effectiveness. Objective In this study, we evaluated the antimicrobial activity of 35 widely available mouth rinses against bacterial species involved in initiation of dental biofilm – Streptococcus gordonii, Streptococcus mitis, Streptococcus oralis, Streptococcus salivarius, and Streptococcus sanguinis. Material and method The Minimum Inhibitory Concentration (MIC) and the Minimum Bactericidal Concentration (MBC) of the evaluated mouth rinses were determined according to the Clinical & Laboratory Standards Institute protocols. Data were submitted to Kruskal-Wallis test and Mann-Whitney post hoc (α=0.05). Result About 70% of the mouth rinses achieved high antibacterial activity and 30%, a low antibacterial activity against all the species tested. The most ineffective mouth rinse showed antibacterial activity (MIC) at 1:1 dilution, while the most effective showed activity even at 1:2048 dilution, which may imply prolonged effect in the mouth. About 51% of mouth rinses showed bactericidal activity, and it was verified that cetylpyridinium chloride or chlorhexidine digluconate containing in the formulation were associated with the highest activity. Conclusion Most - but not all - mouth rinses commercially available are effective in inhibiting in vitro initial colonizers of dental surfaces.

scholarly journals Unveiling the Mechanism of Action of 7α-acetoxy-6β-hydroxyroyleanone on an MRSA/VISA Strain: Membrane and Cell Wall Interactions

Biomolecules ◽  
2020 ◽  
Vol 10 (7) ◽  
pp. 983
Author(s):  
Filipe Pereira ◽  
Teresa Figueiredo ◽  
Rodrigo F. M. de Almeida ◽  
Catarina A. C. Antunes ◽  
Catarina Garcia ◽  
...  
Keyword(s):  
Cell Wall ◽  
Antibacterial Activity ◽  
Lipid Bilayers ◽  
Mechanism Of Action ◽  
Resistant Bacteria ◽  
High Antibacterial Activity ◽  
Cell Wall Disruption ◽  
Low Cytotoxicity ◽  
Mrsa Strains ◽  
Interesting Alternative

The number of cases of failure in the treatment of infections associated with resistant bacteria is on the rise, due to the decreasing efficacy of current antibiotics. Notably, 7α-Acetoxy-6β-hydroxyroyleanone (AHR), a diterpene isolated from different Plectranthus species, showed antibacterial activity, namely against Methicillin-resistant Staphylococcus aureus (MRSA) strains. The high antibacterial activity and low cytotoxicity render this natural compound an interesting alternative against resistant bacteria. The aim of this study is to understand the mechanism of action of AHR on MRSA, using the MRSA/Vancomycin-intermediate S. aureus (VISA) strain CIP 106760, and to study the AHR effect on lipid bilayers and on the cell wall. Although AHR interacted with lipid bilayers, it did not have a significant effect on membrane passive permeability. Alternatively, bacteria treated with this royleanone displayed cell wall disruption, without revealing cell lysis. In conclusion, the results gathered so far point to a yet undescribed mode of action that needs further investigation.

scholarly journals Antibacterial Activities of Prenylated Isoflavones from Maclura tricuspidata against Fish Pathogenic Streptococcus: Their Structure-Activity Relationships and Extraction Optimization

Molecules ◽  
2021 ◽  
Vol 26 (24) ◽  
pp. 7451
Author(s):  
Jae-Woong Lim ◽  
Yang Hee Jo ◽  
Ji-Seok Choi ◽  
Mi Kyeong Lee ◽  
Ki Yong Lee ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Principal Component ◽  
Antibacterial Activities ◽  
Clinical Effects ◽  
Extraction Temperature ◽  
Box Behnken Design ◽  
High Antibacterial Activity ◽  
Low Cytotoxicity ◽  
Zoonotic Bacteria ◽  
Temperature Time

Streptococcus zoonotic bacteria cause serious problems in aquaculture with clinical effects on humans. A structure-antibacterial activity relationships analysis of 22 isoflavones isolated from M. tricuspidata (leaves, ripe fruits, and unripe fruits) against S. iniae revealed that prenylation of the isoflavone skeleton was an important key for their antibacterial activities (minimum inhibitory concentrations: 1.95–500 μg/mL). Through principal component analysis, characteristic prenylated isoflavones such as 6,8-diprenlygenistein (4) were identified as pivotal compounds that largely determine each part’s antibacterial activities. M. tiricuspidata ripe fruits (MTF), which showed the highest antibacterial activity among the parts tested, were optimized for high antibacterial activity and low cytotoxicity on fathead minnow cells using Box–Behnken design. Optimized extraction conditions were deduced to be 50%/80 °C/7.5 h for ethanol concentration/extraction temperature/time, and OE-MTF showed contents of 6,8-diprenlygenistein (4), 2.09% with a MIC of 40 µg/mL. These results suggest that OE-MTF and its active isoflavones have promising potential as eco-friendly antibacterial agents against streptococcosis in aquaculture.

Substituted Furanocoumarins as Novel Class of Antibacterial Translation Inhibitors

2019 ◽  
Vol 22 (6) ◽  
pp. 400-410
Author(s):  
Yan A. Ivanenkov ◽  
Renat S. Yamidanov ◽  
Ilya A. Osterman ◽  
Petr V. Sergiev ◽  
Andrey A. Ayginin ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
High Throughput Screening ◽  
Luciferase Assay ◽  
Cytotoxicity Test ◽  
Reporter System ◽  
Lead Compounds ◽  
High Antibacterial Activity ◽  
Low Cytotoxicity ◽  
Screening Platform

Introduction: A variety of organic compounds has been reported to have antibacterial activity. However, antimicrobial resistance is one of the main problems of current anti-infective therapy, and the development of novel antibacterials is one of the main challenges of current drug discovery. Methods: Using our previously developed dual-reporter High-Throughput Screening (HTS) platform, we identified a series of furanocoumarins as having high antibacterial activity. The construction of the reporter system allows us to differentiate three mechanisms of action for the active compounds: inhibition of protein synthesis (induction of Katushka2S), DNA damaging (induction of RFP) or other (inhibition of bacterial growth without reporter induction). Results: Two primary hit-molecules of furanocoumarin series demonstrated relatively low MIC values comparable to that observed for Erythromycin (Ery) against E. coli and weakly induced both reporters. Dose-dependent translation inhibition was shown using in vitro luciferase assay, however it was not confirmed using C14-test. A series of close structure analogs of the identified hits was obtained and investigated using the same screening platform. Compound 19 was found to have slightly lower MIC value (15.18 µM) and higher induction of Katushka2S reporter in contrast to the parent structures. Moreover, translation blockage was clearly identified using both in vitro luciferase assay and C14 test. The standard cytotoxicity test revealed a relatively low cytotoxicity of the most active molecules. Conclusion: High antibacterial activity in combination with low cytotoxicity was demonstrated for a series of furanocoumarins. Further optimization of the described structures may result in novel and attractive lead compounds with promising antibacterial efficiency.

Green synthesis of silver nanoparticles with high antimicrobial activity and low cytotoxicity using catechol-conjugated chitosan

RSC Advances ◽  
2016 ◽  
Vol 6 (69) ◽  
pp. 64357-64363 ◽  
Author(s):  
Xiaofei Huang ◽  
Yichuan Pang ◽  
Yalan Liu ◽  
Yi Zhou ◽  
Zhengke Wang ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Silver Nanoparticles ◽  
Antibacterial Activity ◽  
Green Synthesis ◽  
High Antimicrobial Activity ◽  
Stabilizing Agent ◽  
Low Cytotoxicity

Catechol-conjugated chitosan was synthesized to act as a reducing and stabilizing agent in the preparation of silver nanoparticles. The resulting silver nanoparticles exhibit strong antibacterial activity and low cytotoxicity.

Synthesis and antibacterial activity of some 1-aryl-1,4-dihydro-4-oxocinnoline-3-carboxylic acids

1990 ◽  
Vol 55 (5) ◽  
pp. 1311-1320 ◽  
Author(s):  
Stanislav Rádl ◽  
Jaroslav Moural ◽  
Radoslava Bendová
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Carboxylic Acids ◽  
Coupling Reaction ◽  
Cyclic Amines ◽  
Nucleophilic Cyclization ◽  
Benzene Diazonium

The coupling reaction of corresponding benzene diazonium chlorides with benzoyl acetates IIIa-IIIc yielded intermediates IVa-IVe. Their intramolecular nucleophilic cyclization provided 1-aryl-1,4-dihydro-4-oxocinnoline-3-carboxylates Va-Ve. Compounds Va, Vb, Vd, and Ve were hydrolyzed to acids VIa-VIc. Treatment of these acids with the respective cyclic amines yielded compounds VIIa-VIIg which were converted to their hydrochlorides. All compounds prepared were tested for their antimicrobial activity in vitro.

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