scholarly journals New Poly(Propylene Imine) Dendrimer Modified with Acridine and Its Cu(II) Complex: Synthesis, Characterization and Antimicrobial Activity

Materials ◽  
2019 ◽  
Vol 12 (18) ◽  
pp. 3020 ◽  
Author(s):  
Paula Bosch ◽  
Desislava Staneva ◽  
Evgenia Vasileva-Tonkova ◽  
Petar Grozdanov ◽  
Ivanka Nikolova ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Copper Ions ◽  
Spectral Characteristics ◽  
Dilution Method ◽  
Pathogenic Microorganisms ◽  
Paramagnetic Resonance ◽  
Poly Propylene ◽  
New Compounds ◽  
First Time

A second-generation poly(propylene imine) dendrimer modified with acridine and its Cu(II) complex have been synthesized for the first time. It has been found that two copper ions form complexes with the nitrogen atoms of the dendrimeric core by coordinate bonds. The new compounds have been characterized by nuclear magnetic resonance (NMR), electron paramagnetic resonance (EPR), fourier-transform infrared spectroscopy (FTIR) and fluorescence spectroscopy. The spectral characteristics of the modified dendrimer have been measured in different organic solvents, and a negative fluorescence solvatochromism has been observed. The antimicrobial activity of the dendrimers has been tested against model pathogenic microorganisms in agar and by broth dilution method. The cotton fabric treated with both dendrimers has been evaluated towards pathogenic microorganisms. The obtained modified cotton fabrics have been shown to hamper bacterial growth and to prevent biofilm formation. Dendrimer cytotoxicity has been investigated in vitro in the model HEp-2 cell line.

scholarly journals Novel Derivatives of 4-Methyl-1,2,3-Thiadiazole-5-Carboxylic Acid Hydrazide: Synthesis, Lipophilicity, and In Vitro Antimicrobial Activity Screening

2021 ◽  
Vol 11 (3) ◽  
pp. 1180
Author(s):  
Kinga Paruch ◽  
Łukasz Popiołek ◽  
Anna Biernasiuk ◽  
Anna Berecka-Rycerz ◽  
Anna Malm ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Carboxylic Acid ◽  
Bacterial Infections ◽  
Acid Hydrazide ◽  
Antimicrobial Effect ◽  
In Vitro Antimicrobial Activity ◽  
Research Goal ◽  
New Compounds ◽  
Derivatives Of

Bacterial infections, especially those caused by strains resistant to commonly used antibiotics and chemotherapeutics, are still a current threat to public health. Therefore, the search for new molecules with potential antimicrobial activity is an important research goal. In this article, we present the synthesis and evaluation of the in vitro antimicrobial activity of a series of 15 new derivatives of 4-methyl-1,2,3-thiadiazole-5-carboxylic acid. The potential antimicrobial effect of the new compounds was observed mainly against Gram-positive bacteria. Compound 15, with the 5-nitro-2-furoyl moiety, showed the highest bioactivity: minimum inhibitory concentration (MIC) = 1.95–15.62 µg/mL and minimum bactericidal concentration (MBC)/MIC = 1–4 µg/mL.

scholarly journals Bactericidal activity of three different antiseptic ophthalmic preparations as surgical prophylaxis

2021 ◽  
Author(s):  
Daniele Tognetto ◽  
Marco R. Pastore ◽  
Gian Marco Guerin ◽  
Giuliana Decorti ◽  
Martina Franzin ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Povidone Iodine ◽  
Bacterial Load ◽  
Viable Cells ◽  
Polyethylene Glycol 1000 ◽  
Oil Concentration ◽  
Short Time ◽  
First Time ◽  
Antiseptic Solutions

Abstract Purpose In the era of antibiotic resistance, there is an increased interest in antiseptic solutions that might represent a reliable option for ocular surface disinfection. The objective of this study is to compare for the first time three different antiseptic ophthalmic preparations to assess their in vitro antimicrobial activity. Methods The antiseptic activity of three commercial ophthalmic solutions, IODIM (povidone-iodine 0.6% in hyaluronic acid vehicle—Medivis, Catania, Italy), OZODROP (nanoemulsion with ozonated oil—concentration not specified—FBVision, Ophthalmic Pharmaceuticals, Rome, Italy), and DROPSEPT (chlorhexidine 0.02% and vitamin E 0.5% Tocopherol Polyethylene Glycol 1000 Succinate—TPGS, Sooft Italia, Montegiorgio, Italy), was tested in vitro on six reference strains by time-killing assays. Viable cells were evaluated after 1, 15, 30 min; 2, 6, and 24 h exposure by seeding 100 µl of the suspension (or appropriate dilutions) on LB agar or Sabouraud-dextrose agar. All plates were incubated at 37 °C for 24 h and evaluated by manually counting the colonies. Results IODIM solution showed a very rapid microbicidal activity: the number of viable cells for all the tested strains was under the detection limit (less than 10 CFU/ml) already after 1 min exposure, and this result was maintained at every incubation time. The rapid antimicrobial activity of povidone-iodine was not replicated when testing the other two antiseptics. Conclusions The study reports the great efficacy in reducing bacterial load in a very short time of povidone-iodine 0.6% compared with other antiseptic preparations.

scholarly journals Nitrogen and Bromide Co-Doped Hydroxyapatite Thin Films with Antimicrobial Properties

Coatings ◽  
2021 ◽  
Vol 11 (12) ◽  
pp. 1505
Author(s):  
Simona Liliana Iconaru ◽  
Carmen Steluta Ciobanu ◽  
Daniela Predoi ◽  
Mikael Motelica-Heino ◽  
Constantin Cătălin Negrilă ◽  
...  
Keyword(s):  
Thin Films ◽  
Antimicrobial Activity ◽  
Spin Coating ◽  
Thin Layers ◽  
Precipitation Method ◽  
X Ray ◽  
Co Precipitation ◽  
First Time ◽  
Co Doped

Hydroxyapatite (Ca10(PO4)6(OH)2, HAp), due to its high biocompatibility, is widely used as biomaterial. Doping with various ions of hydroxyapatite is performed to acquire properties as close as possible to the biological apatite present in bones and teeth. In this research the results of a study performed on thin films of hydroxyapatite co-doped with nitrogen and bromine (NBrHAp) are presented for the first time. The NBrHAp suspension was obtained by performing the adapted co-precipitation method using cetyltrimethylammonium bromide (CTAB). The thin layers of NBrHAp were obtained by spin-coating. The stability of the NBrHAp suspension was examined by ultrasound measurements. The thin layers obtained by the spin-coating method were examined by scanning electron microscopy (SEM), optical microscopy (OM), and metallographic microscopy (MM). The presence of nitrogen and bromine were highlighted by energy-dispersive X-ray spectroscopy (EDS) and X-ray photoelectron spectroscopy (XPS) studies. Fourier transform infrared spectroscopy (FTIR) was used to highlight the chemical status of nitrogen and bromine. In addition, the powder obtained from the NBrHAp suspension was analyzed by XRD. Moreover, the in vitro antimicrobial activity of the NBrHAp suspensions and coatings was investigated using the reference microbial strains Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, and Candida albicans ATCC 10231. The results highlighted the successful obtainment of N and Br co-doped hydroxyapatite suspension for the first time by an adapted co-precipitation method. The obtained suspension was used to produce pure NBrHAp composite thin films with superior morphological properties. The NBrHAp suspensions and coatings exhibited in vitro antimicrobial activity against bacterial and fungal strains and revealed their good antimicrobial activity.

scholarly journals ANTIMICROBIAL ACTIVITY STUDY OF NEW QUINAZOLIN-4(3H)-ONES AGAINST STAPHYLOCOCCUS AUREUS AND STREPTOCOCCUS PNEUMONIAE

2021 ◽  
Vol 9 (4) ◽  
pp. 318-329
Author(s):  
M. A. Samotrueva ◽  
A. A. Ozerov ◽  
A. A. Starikova ◽  
N. M. Gabitova ◽  
D. V. Merezhkina ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Streptococcus Pneumoniae ◽  
Active Sites ◽  
Wide Spectrum ◽  
Experimental Studies ◽  
Amide Group ◽  
Pharmacological Effect ◽  
Dilution Method

Quinazolin-4(3H)-one derivatives exhibiting a wide spectrum of a pharmacological activity, represent a promising class of substances used to obtain antibacterial agents, which is especially important in the context of the emergence of pathogenic microorganisms’ resistance to drugs used in medicine. It has been proved that compounds having a naphthyl radical in the molecule, as well as an amide group bound to the benzene ring as quinazolinone substituents, are characterized by a pronounced antimicrobial activity against Staphylococcus aureus and Streptococcus pneumoniae.The aim of the research is a primary microbiological screening of the in vitro antimicrobial activity of new quinazolin-4(3H)-one derivatives against Staphylococcus aureus and Streptococcus pneumoniae, as well as the assessment of the relationship between the pharmacological effect and the structural transformation of the substance molecule, lipophilicity and the possibility of forming resistance to them.Materials and methods. The experimental studies have been carried out using well-known nosocomial pathogens of infectious and inflammatory diseases Staphylococcus aureus and Streptococcus pneumoniae by a serial dilution method.Results. A compound containing a naphthyl radical in its structure, which contributes to an increase in the hydrophobicity of the substance and its solubility in the membrane of a bacterial cell, has a bacteriostatic effect against both Staphylococcus aureus and Streptococcus pneumoniae. A similar pharmacological effect is exhibited by a derivative with an amide group as a substituent of the quinazolinone nucleus linked to a phenyl radical, which probably contributes to an increase in the degree of binding to active sites of enzymes involved in the DNA replication, and protein synthesis. Obviously, the increased lipophilicity, which promotes better binding to the efflux protein, cannot serve as objective characteristics of the emergence possibility of the pathogen’s resistance to this substance.Conclusion. Among the synthesized compounds, the leading substances that exhibit an antimicrobial activity against Staphylococcus aureus and Streptococcus pneumonia, have been identified. The assessment of the chemical structure made it possible to substantiate their pharmacological action and draw conclusions about the possibility of developing resistance to it in microbial cells.

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 Cytotoxic, antioxidant, and antimicrobial activities of Celery (Apium graveolens L.)

2021 ◽  
Vol 17 (1) ◽  
pp. 147-156
Author(s):  
Mohammed Saleh Al Aboody ◽  
Keyword(s):  
Antimicrobial Activity ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Antihypertensive Agents ◽  
Apium Graveolens ◽  
Cell Protein ◽  
Dilution Method ◽  
Local Market ◽  
Antioxidant And Antimicrobial Activity

Celery (Apium graveolens Linn, Family: Apiaceae) is a common edible herb used as a spice in the traditional medicine of several nations since time immemorial. The whole plant is extensively used in cooking as soups and salads. A. graveolens has various pharmacological properties such as anticancer, anti-obesity, anti-hepatotoxic, and antihypertensive agents. Hence, it is of interest to document the in vitro cytotoxic, antioxidant, and antimicrobial activity of A. graveolens. The plants were collected in the local market, shade dried, and different parts of the plants were extracted with 70% ethanol using a cold maceration process. Antioxidant tests were performed based on the various radical scavenging methods. Antimicrobial activity and MIC were completed using the respective cup-plate and two-fold serial dilution method. In vitro cytotoxic studies were achieved by the MTT; Sulphorhodamine B assayed total cell protein content. DLA and ESC cells determined the short-term toxicity. The leaf extract exhibited significant antioxidant properties against NO, DPPH, ABTS, LPO, and HPO methods. Thus, potential inhibition against Gram-positive, Gram-negative, and fungal strains within the MIC ranges of 250-500 μg/ml was observed. All the extracts of the plant presented in the study revealed greater cytotoxicity effects against five respective cancer cell lines, L6, Vero, BRL 3A, A-549, L929, and L-929 with the ranging of 443-168.5 μg/ml. Thus, we show that A. graveolens possess a potential cytotoxic, antioxidant, and antimicrobial activity.

scholarly journals Criblage phytochimique et activité antimicrobienne de six rhizomes comestibles utilisés en médecine traditionnelle à Lubumbashi (RDC)

2020 ◽  
Vol 14 (4) ◽  
pp. 1367-1380
Author(s):  
Valentin Chiribagula Bashige ◽  
Amuri Salvius Bakari ◽  
Philippe Ndjolo Okusa ◽  
Emery Mutombo Kalonda ◽  
Jean Baptiste Simbi Lumbu
Keyword(s):  
Antimicrobial Activity ◽  
Traditional Medicine ◽  
Trichophyton Rubrum ◽  
Imperata Cylindrica ◽  
Activité Antibactérienne ◽  
Dilution Method ◽  
Phytochemical Screening ◽  
Chemical Screening ◽  
Médecine Traditionnelle

Les affections microbiennes constituent des pathologies dominantes en RDC où pour y faire face la population recourt aux plantes. Cette étude a été conduite en vue d’évaluer l’activité antimicrobienne et identifier des groupes phytochimiques à potentiel antimicrobien de six rhizomes comestibles, utilisées en médecine traditionnelle à Lubumbashi. Le criblage phytochimique réalisé par des réactions classiques en solution a permis d’identifier dans tous les rhizomes, des flavonoïdes, des saponines, des tannins et dans 66,7% d’entre eux, des quinones et des terpénoïdes. La méthode de dilution a permis d’évaluer l’activité antibactérienne des extraits aqueux (EAQ) et méthanoliques (EME) qui ont tous été actif avec une intensité allant de très forte (CMI = 1,7 μg/mL) à moyenne (CMI = 50 μg/mL). Eriosema verdikii (EME : CMI = 1,7 μg/mL sur N. meningitidis et S. aureus) a présenté la meilleure activité antibactérienne et Imperata cylindrica (EAQ : CMI = 1,7 μg/mL sur Trichophyton rubrum), la meilleure activité antifongique. Le potentiel antimicrobien de ces rhizomes mis en évidence in vitro dans cette étude, fait des espèces étudiées des candidates à des investigations approfondies pouvant aboutir à la mise au point des médicaments traditionnels améliorés ou à la découverte de nouvelles molécules antibactériennes.Mots clés : antifongique, antibactérien, criblage chimique, rhizomes comestibles, Lubumbashi. English Title: Phytochemical Screening and Antimicrobial Activity of Six Edible Rhizomes Used in Traditional Medicine in Lubumbashi (DRC)Microbial infections are dominant pathologies in the DRC where, to deal with them, several people resort to plants used in traditional medicine. This assesses the antimicrobial activity of six edible rhizomes used in traditional medicine in the city of Lubumbashi (DRC) and identifies phytochemical groups. Phytochemical screening by solution reactions allowed the identification of flavonoids, saponins and tannins in all rhizomes, and in 66.7% of the rhizomes were found quinones and terpenoids. The dilution method allowed the evaluation of antibacterial activity, aqueous (EAQ) and methanolic (EME) extracts. This varies from very high (MIC = 1.7 μg / mL) to medium (MIC = 50 μg / mL). Eriosema verdikii (EME: MIC = 1.7 μg / mL on N. meningitidis and S. aureus) has the greatest antibacterial in the collection and Imperata cylindrica (EAQ: MIC = 1.7 μg / mL On Trichophyton rubrum), the greatest antifungal activity. The results obtained by this study show that the six rhizomes studied, along with their food virtues, possess antibacterial and antifungal properties that can explain their use in traditional medicine against various conditions; In addition, the various phytochemical groups within them would play an important role in the proven virtues.Keywords: antifungal, antibacterial, chemical screening, edible rhizomes, Lubumbashi  

scholarly journals Antileishmanial Phenylpropanoids from the Leaves ofHyptis pectinata(L.) Poit

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Rosangela A. Falcao ◽  
Patricia L. A. do Nascimento ◽  
Silvana A. de Souza ◽  
Telma M. G. da Silva ◽  
Aline C. de Queiroz ◽  
...  
Keyword(s):  
Rosmarinic Acid ◽  
Bacterial Infections ◽  
Ethanol Extract ◽  
Spectroscopic Methods ◽  
Etoh Extract ◽  
Promastigote Form ◽  
Water Fractions ◽  
New Compounds ◽  
First Time

Hyptis pectinata, popularly known in Brazil as “sambacaitá” or “canudinho,” is an aromatic shrub largely grown in the northeast of Brazil. The leaves and bark are used in an infusion for the treatment of throat and skin inflammations, bacterial infections, pain, and cancer. Analogues of rosmarinic acid and flavonoids were obtained from the leaves ofHyptis pectinataand consisted of two new compounds, sambacaitaric acid (1) and 3-O-methyl-sambacaitaric acid (2), and nine known compounds, rosmarinic acid (3), 3-O-methyl-rosmarinic acid (4), ethyl caffeate (5), nepetoidin A (6), nepetoidin B (7), cirsiliol (8), circimaritin (9), 7-O-methylluteolin (10), and genkwanin (11). The structures of these compounds were determined by spectroscopic methods. Compounds1–5, and7were evaluatedin vitroagainst the promastigote form ofL. braziliensis, and the ethanol extract. The hexane, ethyl acetate, and methanol-water fractions were also evaluated. The EtOH extract, the hexane extract, EtOAc, MeOH:H2O fractions; and compounds1,2and4exhibited antileishmanial activity, and compound1was as potent as pentamidine. In contrast, compounds3,5, and7did not present activity against the promastigote form ofL. braziliensisbelow 100 µM. To our knowledge, compounds1and2are being described for the first time.

scholarly journals Approach for the Synthesis of Potent Antimicrobials Containing Pyrazole, Pyrimidine and Morpholine Analogues

2016 ◽  
Vol 69 ◽  
pp. 87-96 ◽  
Author(s):  
Nisheeth C. Desai ◽  
Bonny Y. Patel ◽  
Bharti P. Dave
Keyword(s):  
Antimicrobial Activity ◽  
Dilution Method ◽  
Mass Spectral ◽  
H Nmr ◽  
Sar Studies ◽  
Mueller Hinton ◽  
Morpholine Derivatives ◽  
Mueller Hinton Broth ◽  
C Nmr

The present study is in the interest of some synthesized novel derivatives containing 4-(1,3-diphenyl-1H-pyrazol-4-yl)-N-(morpholinomethyl)-6-arylpyrimidin-2-amines pooled with different bio-active heterocycles such as pyrazole, pyrimidine and morpholine derivatives. The structures of newly synthesized compounds were elucidated by IR, 1H NMR, 13C NMR and mass spectral data. The synthesized compounds were evaluated for their in vitro antimicrobial activity against different bacterial and fungal strains using Mueller-Hinton Broth dilution method. On the basis of SAR studies, it was observed that the presence of electron withdrawing groups remarkably enhanced the antimicrobial activity of synthesized compounds.

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