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.

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.

scholarly journals An In Vitro Study on the Antimicrobial Properties of Essential Oil Modified Resin Composite against Oral Pathogens

Materials ◽  
2020 ◽  
Vol 13 (19) ◽  
pp. 4383
Author(s):  
Barbara Lapinska ◽  
Aleksandra Szram ◽  
Beata Zarzycka ◽  
Janina Grzegorczyk ◽  
Louis Hardan ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Resin Composite ◽  
Antimicrobial Properties ◽  
In Vitro Study ◽  
Diffusion Method ◽  
Oral Pathogens

Modifying the composition of dental restorative materials with antimicrobial agents might induce their antibacterial potential against cariogenic bacteria, e.g., S.mutans and L.acidophilus, as well as antifungal effect on C.albicans that are major oral pathogens. Essential oils (EOs) are widely known for antimicrobial activity and are successfully used in dental industry. The study aimed at evaluating antibacterial and antifungal activity of EOs and composite resin material (CR) modified with EO against oral pathogens. Ten EOs (i.e., anise, cinnamon, citronella, clove, geranium, lavender, limette, mint, rosemary thyme) were tested using agar diffusion method. Cinnamon and thyme EOs showed significantly highest antibacterial activity against S.mutans and L.acidophilus among all tested EOs. Anise and limette EOs showed no antibacterial activity against S.mutans. All tested EOs exhibited antifungal activity against C.albicans, whereas cinnamon EO showed significantly highest and limette EO significantly lowest activity. Next, 1, 2 or 5 µL of cinnamon EO was introduced into 2 g of CR and microbiologically tested. The modified CR showed higher antimicrobial activity in comparison to unmodified one. CR containing 2 µL of EO showed the best antimicrobial properties against S.mutans and C.albicans, while CR modified with 1 µL of EO showed the best antimicrobial properties against L.acidophilus.

scholarly journals A new group of compounds derived from 4-, 5-, 6- and 7-aminoindoles with antimicrobial activity

2018 ◽  
Vol 4 (3) ◽  
pp. 27-36 ◽  
Author(s):  
Irina Stepanenko ◽  
Semen Yamashkin ◽  
Yuliya Kostina ◽  
Alyona Batarsheva ◽  
Mikhail Mironov
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antibiotic Resistance ◽  
Biologically Active ◽  
Diffusion Method ◽  
Significant Activity ◽  
Clinical Strains ◽  
Causative Agents ◽  
New Compounds

Introduction. The problem of antibiotic resistance of microorganisms is becoming more urgent in the twenty-first century. Microorganisms possess an evolutionary adaptive capacity. Non-adherence to the basic principles of rational antibiotic therapy leads to menacing consequences. More and more pathogenic microbes are becoming resistant to two or more antibiotics. The search for new compounds with antimicrobial activity is one of the principles for overcoming the antibiotic resistance of microorganisms. Materials and methods. Eighteen test-strains of microorganisms and more than 2000 clinical strains of microorganisms, representating the families Micrococcaceae, Streptococcaceae, Enterobacteriaceae, Moraxellaceae, Pseudomonadaceae, Sphingomonadaceae, Xanthomonadaceae were studied for sensitivity to the compounds derived from 4-, 5-, 6- and 7-aminoindoles. A method of serial dilutions to determine the minimal inhibitory concentration (MIC) of the compounds under study was used in the study, as well as a disc diffusion method. Results and discussion. Sensitivity of the test-strains and of clinical strains of microorganisms to the resulting compounds was studied. The compounds based on substituted 4-, 5-, 6-, 7-aminoindoles showed different activity against the test strains and experimental strains of microorganisms in vitro. It was found that the marked antibacterial activity was exhibited by the compounds containing a trifluoromethyl group. The most significant activity was noted in amides and pyrroloquinolones based on 4-aminoindole, 6-aminoindole and 7-aminoindole.The most effective compounds with laboratory codes 5D, 7D, 39D, S3, HD, 4D showed a pronounced antibacterial activity. Conclusion. Antimicrobial activity of the substituted amides and pyrroloquinolines on the basis of 4-, 5-, 6-, 7-aminoindoles was etermined in our study, as well as the spectra of their action against Gram-positive and Gram-negative microorganisms, which are causative agents of non-specific and certain specific human infectious diseases. Moreover, we evaluated the synthetic potentials of the substituted 4-, 5-, 6-, 7-aminoindoles as the starting compounds for synthesizing a series of indolylamides and pyrroloquinolines. Also, the prospects for targeted synthesis of biologically active compounds based on indole-type aromatic amines were determined.

scholarly journals Cytocompatibility and Antibacterial Properties of Capping Materials

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Claudio Poggio ◽  
Carla Renata Arciola ◽  
Riccardo Beltrami ◽  
Annachiara Monaco ◽  
Alberto Dagna ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antibacterial Properties ◽  
Disc Diffusion ◽  
Streptococcus Salivarius ◽  
Diffusion Test ◽  
Streptococcus Sanguis ◽  
Agar Disc ◽  
Bacterial Growth Inhibition

The aim of this study was to evaluate and compare the antimicrobial activity and cytocompatibility of six different pulp-capping materials: Dycal (Dentsply), Calcicur (Voco), Calcimol LC (Voco), TheraCal LC (Bisco), MTA Angelus (Angelus), and Biodentine (Septodont). To evaluate antimicrobial activity, materials were challengedin vitrowithStreptococcus mutans,Streptococcus salivarius, andStreptococcus sanguisin the agar disc diffusion test. Cytocompatibility of the assayed materials towards rat MDPC-23 cells was evaluated at different times by both MTT and apoptosis assays. Results significantly differed among the different materials tested. Both bacterial growth inhibition halos and cytocompatibility performances were significantly different among materials with different composition. MTA-based products showed lower cytotoxicity and valuable antibacterial activity, different from calcium hydroxide-based materials, which exhibited not only higher antibacterial activity but also higher cytotoxicity.

Evaluation of Antibacterial Activity of Combined Plant Extract of Pyracantha crenulata and Zanthoxylum armatum

2020 ◽  
Vol 2 (29) ◽  
pp. 32-36
Author(s):  
Semwal Amit Negi Sweta
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Ethanolic Extract ◽  
Diffusion Method ◽  
Moderate Activity ◽  
Aqueous Extracts ◽  
Disk Diffusion Method ◽  
Zanthoxylum Armatum ◽  
Plant Extraction

Abstract-Medicinal plants represent an essential source of drugs and have played an important role in healthcaresystem.PyracanthacrenulataandZanthoxylum armatumhave been used as traditional medicine. The main aim of the study was to find the antibacterial activity of the selected plants against bacterialspecies:E.coliandPseudomonasaeruginosa. The solvents used for plant extraction were hexane, chloroform, ethanol and aqueous. The in vitro antimicrobial activity was performed by Agar disk diffusion method. The hexane and aqueous extracts showed moderate activity whereas theethanolicextractsshowedasignificantantibacterial activity. In the study Tetracycline was used as standard. The combined ethanolic extract of both the selected plant showed the synergistic effect on the bacterial strain tested. This leads to the conclusion that the combined effect can have possible application in the development of products as antimicrobial.

In Vitro Studies of Antibacterial Activity of Bioglasses Releasing Ag+

2011 ◽  
Vol 493-494 ◽  
pp. 108-113
Author(s):  
Lidia Ciołek ◽  
Joanna Karaś ◽  
Andrzej Roman Olszyna ◽  
Ewa Zaczyńska ◽  
Anna Czarny ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Surgical Treatment ◽  
Micro Organisms

The research of obtained bioglasses in the form of silver-containing powders were presented in this paper. The research conducted in order to determine antimicrobial activity under in vitro conditions of bioglasses. The results confirmed that these bioglasses Z-5, Z-8 and B-I inhibit the growth of most micro-organisms during the tested period and could be used in surgical treatment of the most advanced parodontium illnesses.

Synthesis and In Vitro Antibacterial Activity of Some 1-(Difluoromethoxyphenyl)quinolone-3-carboxylic Acids

1989 ◽  
Vol 78 (7) ◽  
pp. 585-588 ◽  
Author(s):  
W. Xiao ◽  
R. Krishnan ◽  
Y.-I. Lin ◽  
E.F. Delos Santos ◽  
N.A. Kuck ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Carboxylic Acids ◽  
In Vitro Antibacterial Activity

scholarly journals In Vitro Antimicrobial Activity Evaluation of a Novel Fitostimoline® Plus Spray Formulation

2021 ◽  
Vol 2021 ◽  
pp. 1-7
Author(s):  
Maria Domenica Falciglia ◽  
Roberta Palladino ◽  
Barbara Maglione ◽  
Giulia Schiavo
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Standard Of Care ◽  
Microbial Infection ◽  
In Vitro Antimicrobial Activity ◽  
Disk Diffusion Assay ◽  
Spray Formulation ◽  
Carrier Test ◽  
And Control

Wound contaminants are the main cause of healing delay and infection in both chronic and acute wounds; for this reason, the microbial infection management in wound healing is one of the most important components for an effective standard of care. The wound contaminants are most likely to originate from the environment and from the surrounding skin lesion, and to date, the most frequent bacteria isolated are Staphylococcus aureus, Pseudomonas aeruginosa, and Klebsiella pneumoniae. In order to counteract and control these contaminants, the standard care includes topical antiseptic agents. The most commonly used include iodine-releasing agents (e.g., povidone-iodine), hydrogen peroxide, and polyhexanide. This study aims to investigate the in vitro antibacterial activity of a novel topical spray (Fitostimoline® Plus spray) based on 0.1% polyhexanide and Rigenase® against S. aureus, P. aeruginosa, K. pneumoniae, and the combination of S. aureus and K. pneumoniae. The in vitro antimicrobial activity of Fitostimoline® Plus spray was evaluated by the agar disk diffusion assay, quantitative suspension test, and quantitative carrier test, demonstrating that Fitostimoline® Plus spray is able to kill 99.9% bacteria. These results support the microbiological characterization of Fitostimoline® Plus spray confirming the antibacterial activity of polyhexanide (PHMB).

scholarly journals In-vitro Callogenesis and Screening of Antimicrobial Activity of Callus and Seed of Caesalpinia bonducella F.: A Threatened Medicinal Plant of Western Ghats

2021 ◽  
pp. 76-89
Author(s):  
Rajani Shirsat ◽  
Ajit Kengar ◽  
Aruna Rai
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Plant Growth ◽  
Medicinal Plant ◽  
Plant Growth Regulators ◽  
Growth Regulators ◽  
Western Ghats ◽  
Callus Formation ◽  
Caesalpinia Bonducella

Aim: Caesalpinia bonducella Flem is a dioecious scrambling woody liana of Caesalpinoideae, a subfamily of Leguminosae. The plant is threatened and distributed in the deciduous forests of the Western Ghats of India. Being an important medicinal plant Caesalpinia bonducella F. attracted many scientists to exploit various activities associated with a number of phytoconstituents. The present study was undertaken to evaluate the most suitable media and suitable concentrations of plant growth regulators for in vitro Callogenesis and screening of antimicrobial activity of callus and seed of Caesalpinia bonducella. Materials and Methods: Callus was initiated from stem explants, on 1x and 0.5x MS medium plus supplements. The effects of plant growth regulators on callus cultures were studied and observations were made. The in vitro antibacterial activity was performed by using extracts of callus and seed of Caesalpinia bonducella in petroleum ether and methanol against multidrug resistance organisms. The organic extracts of seed and callus of the plant at concentrations of 0.02 mg/ml - 0.1 mg/ml were taken and their activities were measured.   Results: The combination of 2.5 mgL-1 2,4-D  with 2 mgL-1 BAP, resulted in the highest frequency and the highest mean percentage of callus formation (2.35 ± 0.294) with yellow friable callus. The results revealed that all the extracts had a variable degree of antibacterial activity. Conclusions: It was observed that 2,4-D at 2.5 mgL-1 in combination with BAP,2.0 mgL-1 BAP resulted in early initiation, highest induction percentage, with frequency highest mean percentage of callus formation, Antimicrobial tests with methanol and diethyl ether extract of Caesalpinia bonducella seed powder against the clinical isolates showed the zone of inhibition for all the pathogens tested with concentration of methanolic extract of C. bonducella seed powder.

scholarly journals Maclura tinctoria Extracts: In Vitro Antibacterial Activity against Aeromonas hydrophila and Sedative Effect in Rhamdia quelen

Fishes ◽  
2021 ◽  
Vol 6 (3) ◽  
pp. 25
Author(s):  
Luana da Costa Pires ◽  
Patricia Rodrigues ◽  
Quelen Iane Garlet ◽  
Luisa Barichello Barbosa ◽  
Bibiana Petri da Silveira ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Phenolic Compounds ◽  
Pathogenic Bacteria ◽  
Sedative Effect ◽  
In Vitro Antimicrobial Activity ◽  
Normal Behavior ◽  
In Vitro Antibacterial Activity ◽  
Light Sedation

Maclura tinctoria is a tree species native from Brazil and rich in phenolic compounds. Since plant antibacterial activity is highly associated with phenolic compound concentration, we aim to evaluate the in vitro antimicrobial activity of different extracts against fish pathogenic bacteria. In addition, some phenolic compounds have central depressant effects and can be useful in aquaculture due to possible sedative and/or anesthetic effects. Four M. tinctoria extracts were extracted separately with ethanol; leaves (LE), bark (BE), heartwood (HE), and the sapwood (SE). In vitro antimicrobial activity was tested against Aeromonas strains at concentrations of 6400 to 3.125 μg/mL. The sedative effect was evaluated for 24 h with 30 and 100 mg/L concentrations. Chemical composition was analyzed by HPLC-DAD-MS. The HE extract had the best MIC (400 µg/mL) and MBC (800 µg/mL) compared to the LE, BE, and SE extracts. LE extract induced deep sedation and the BE, SE, and HE extracts induced light sedation. Additionally, BE, SE, and HE induced a normal behavior without side effects. Polyphenolic compounds with antimicrobial activity and sedative effects were identified mainly in HE. Thus, HE extract is safe and can be used as a sedative for silver catfish.

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