scholarly journals Synthesis, Antibacterial and Cytotoxic Activities of New Thiazole Based Pyrrolidine Derivatives

2021 ◽  
Vol 11 (4) ◽  
pp. 12178-12185
Keyword(s):  
Mammalian Cells ◽  
Antibacterial Activities ◽  
Cytotoxic Activities ◽  
Spectroscopic Techniques ◽  
Phenyl Derivative ◽  
Gram Positive Bacteria ◽  
Microdilution Method ◽  
Cytotoxicity Studies ◽  
Broth Microdilution Method ◽  
Ft Ir

In this study, some thiazole-based pyrrolidine derivatives were synthesized, characterized by FT-IR and 1H NMR spectroscopic techniques, and evaluated as potential antibacterial agents. Their antibacterial activities were evaluated by broth microdilution method and expressed as minimum inhibitory concentration; against Escherichia coli, Salmonella typhimurium, Bacillus cereus, and Staphylococcus aureus. Cytotoxicity studies of synthesized compounds were also conducted to minimize the toxic effects on healthy mammalian cells. From synthesized compounds, 4-F-phenyl derivative compound (11) has been found to inhibit Gram-positive bacteria with minimum toxicity selectively.

Synthesis, Characterization and X-Ray Crystal Structure of the New Schiff Base and Anticandidal Evaluation

2019 ◽  
Vol 41 (6) ◽  
pp. 1090-1090
Author(s):  
Mehmet Poyraz Mehmet Poyraz ◽  
Musa Sari Musa Sari ◽  
Halil Berber Halil Berber ◽  
Nursenem Karaca and Fatih Demirci Nursenem Karaca and Fatih Demirci
Keyword(s):  
Schiff Base ◽  
Spectroscopic Techniques ◽  
X Ray Diffraction ◽  
X Ray ◽  
Microdilution Method ◽  
Broth Microdilution Method ◽  
Ft Ir ◽  
Anticandidal Activity ◽  
Crystal Structural

A new Schiff base, namely 2-methoxy-6-((2-(4 nitrophenyl) hydrazineylidene) methyl)phenol was synthesized and characterized by melting points, elemental analysis, thermogravimetric analysis and spectroscopic techniques (FT-IR, 1H-NMR and UV-VIS spectra). The chemical structure of compound was further confirmed by single crystal structural X-ray diffraction. The Schiff base is crystallized in the triclinic space group P-1. In the crystal, molecules are linked by O-H…O hydrogen bonds between the hydroxy “-O-” atom and the methoxy “-O-” atom. Furthermore, the synthesized Schiff base was tested for the in vitro anticandidal activities using CLSI broth microdilution method against human pathogenic Candida albicans, C. parapsilosis and C. krusei standard strains. In the anticandidal activity test results, the new Schiff base was found to be effective at 1 mg/mL - 0.25 mg/mL concentrations. (The last line omitted) (The sentence marked in red will be deleted)

scholarly journals Hetero-Binuclear Complexes of Lanthanum (III) Using Bridging N,N′-Bis(2-Pyridylmethyl)Oxamide and Terminal 1,10-Phenanthroline: Synthesis, Characterization and Biological Evaluation

2018 ◽  
Vol 10 (6) ◽  
Author(s):  
P. R. Chetana ◽  
Vibha Vinayakumar Bhat ◽  
Mohan A. Dhale
Keyword(s):  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Antibacterial Activities ◽  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
Spectroscopic Techniques ◽  
Binuclear Complexes ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Chemical Nuclease

In the present study, hetero-binuclear La(III) complexes were newly synthesized using well known bridging ligand N,N′-bis(2-pyridylmethyl)oxamide (2PMO, 1) and “complexes as ligands” [Cu(2PMO)] (2) and [Ni(2PMO)] (3). The newly synthesized mononuclear (4) as well as hetero-binuclear complexes (5 and 6) were characterized by analytical and spectroscopic techniques. The newly synthesized complexes were tested for their binding ability towards CT-DNA and chemical nuclease property towards SC pUC 19 DNA. The complexes were tested for antibacterial activities against Gram negative bacteria (E. coli and K. pneumonia) and Gram positive bacteria (B. subtilis and S. aureus), antioxidant activities by DPPH radical scavenging and ferrous-ion chelation methods and cytotoxicity against MCF-7 cell lines by MTT assay. The structure-activity relationship revealed that the newly synthesized hetero-binuclear complexes show potent DNA binding and chemical nuclease activities, antibacterial, antioxidant and cytotoxic activities.

scholarly journals Multifunctional application of PVA-aided Zn–Fe–Mn coupled oxide nanocomposite

2021 ◽  
Vol 16 (1) ◽  
Author(s):  
Buzuayehu Abebe ◽  
H. C. Ananda Murthy ◽  
Enyew Amare Zereffa
Keyword(s):  
Charge Transfer ◽  
Analytical Techniques ◽  
Antibacterial Activities ◽  
Poly Vinyl Alcohol ◽  
Blue Dye ◽  
Ternary Oxide ◽  
Gram Positive Bacteria ◽  
Transfer Capability ◽  
Ft Ir ◽  
Synthesized Materials

AbstractZinc oxide (ZnO) is a fascinating semiconductor material with many applications such as adsorption, photocatalysis, sensor, and antibacterial activities. By using a poly (vinyl alcohol) (PVA) polymer as a capping agent and metal oxides (iron and manganese) as a couple, the porous PVA-aided Zn/Fe/Mn ternary oxide nanocomposite material (PTMO-NCM) was synthesized. The thermal, optical, crystallinity, chemical bonding, porosity, morphological, charge transfer properties of the synthesized materials were confirmed by DTG/DSC, UV–Vis-DRS, XRD, FT-IR, BET, SEM-EDAX/TEM-HRTEM-SAED, and CV/EIS/amperometric analytical techniques, respectively. The PTMO-NCM showed an enhanced surface area and charge transfer capability, compared to ZnO. Using the XRD pattern and TEM image analysis, the crystalline size of the materials was confirmed to be in the nanometer range. The porosity and superior charge transfer capabilities of the PTMO-NCM were confirmed from the BET, HRTEM (IFFT)/SAED, and CV/EIS analysis. The adsorption kinetics (adsorption reaction/adsorption diffusion) and adsorption isotherm test confirmed the presence of a chemisorption type of adsorbate/methylene blue dye-adsorbent/PTMO-NCM interaction. The photocatalytic performance was tested on the Congo red and Acid Orange-8 dyes. The superior ascorbic acid sensing capability of the material was understood from CV and amperometric analysis. The noble antibacterial activities of the material were also confirmed on both gram-negative and gram-positive bacteria.

Synthesis and Antibacterial Activities of Amidine Substituted Monocyclic β-Lactams

2021 ◽  
Vol 17 ◽  
Author(s):  
Lijuan Zhai ◽  
Lili He ◽  
Yuanbai Liu ◽  
Ko Ko Myo ◽  
Zafar Iqbal ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Bacterial Species ◽  
Antimicrobial Effect ◽  
Antibacterial Activities ◽  
Lead Target ◽  
Bacterial Strains ◽  
Microdilution Method ◽  
Broth Microdilution Method ◽  
Clinical Interest

Background: Mononcyclic β-lactams are regarded as the most resistant class of β-lactams against a series of β-lactamases though possess limited antibacterial activity. Aztreonam being the first clinically approved monobactam needs broad-spectrum efficacy through structural modification. Objective: We strive to synthesize a number of monocyclic β-lactams by varying the substituents at N1, C3 and C4 positions of azetidinone ring and study the antimicrobial effect on variable bacterial strains. Methods: Seven new monobactam derivatives 23a-g, containing substituted-amidine moieties linked to the azetidinone ring via thiazole linker, were synthesized through multistep synthesis. The final compounds were investigated for their in vitro antibacterial activities using broth microdilution method, against ten bacterial strains of clinical interest. The minimum inhibitory concentrations (MICs) of newly synthesized derivatives were compared with aztreonam, ceftazidime and meropenem, existing clinical antibiotics. Results: All compounds 23a-g showed higher antibacterial activities (MIC 0.25 µg/mL to 64 µg/mL) against tested strains as compared to aztreonam (MIC 16 µg/mL to >64 µg/mL) and ceftazidime (MIC >64 µg/mL). However all compounds, except 23d, exhibited lower antibacterial activity against all tested bacterial strains as compared to meropenem. Conclusion: Compound 23d showed comparable or improved antibacterial activity (MIC 0.25 µg/mL to 2 µg/mL) to meropenem (MIC 1 µg/mL to 2 µg/mL) in case of seven bacterial species. Therefore, compound 23d may be valuable lead target for further investigations against multi-drug resistant Gram-negative bacteria.

scholarly journals In Vitro Activity of Eravacycline against Gram-Positive Bacteria Isolated in Clinical Laboratories Worldwide from 2013 to 2017

2019 ◽  
Vol 64 (3) ◽  
Author(s):  
Ian Morrissey ◽  
Stephen Hawser ◽  
Sibylle H. Lob ◽  
James A. Karlowsky ◽  
Matteo Bassetti ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Clinical Isolates ◽  
Gram Positive ◽  
Content Type ◽  
Gram Positive Bacteria ◽  
Microdilution Method ◽  
Clinical Laboratories ◽  
Broth Microdilution Method ◽  
Doubling Dilution

ABSTRACT Eravacycline is a novel, fully synthetic fluorocycline antibiotic being developed for the treatment of serious infections, including those caused by resistant Gram-positive pathogens. Here, we evaluated the in vitro activities of eravacycline and comparator antimicrobial agents against a recent global collection of frequently encountered clinical isolates of Gram-positive bacteria. The CLSI broth microdilution method was used to determine in vitro MIC data for isolates of Enterococcus spp. (n = 2,807), Staphylococcus spp. (n = 4,331), and Streptococcus spp. (n = 3,373) isolated primarily from respiratory, intra-abdominal, urinary, and skin specimens by clinical laboratories in 37 countries on three continents from 2013 to 2017. Susceptibilities were interpreted using both CLSI and EUCAST breakpoints. There were no substantive differences (a >1-doubling-dilution increase or decrease) in eravacycline MIC90 values for different species/organism groups over time or by region. Eravacycline showed MIC50 and MIC90 results of 0.06 and 0.12 μg/ml, respectively, when tested against Staphylococcus aureus, regardless of methicillin susceptibility. The MIC90 values of eravacycline for Staphylococcus epidermidis and Staphylococcus haemolyticus were equal (0.5 μg/ml). The eravacycline MIC90s for Enterococcus faecalis and Enterococcus faecium were 0.06 μg/ml and were within 1 doubling dilution regardless of the vancomycin susceptibility profile. Eravacycline exhibited MIC90 results of ≤0.06 μg/ml when tested against Streptococcus pneumoniae and beta-hemolytic and viridans group streptococcal isolates. In this surveillance study, eravacycline demonstrated potent in vitro activity against frequently isolated clinical isolates of Gram-positive bacteria (Enterococcus, Staphylococcus, and Streptococcus spp.), including isolates collected over a 5-year period (2013 to 2017), underscoring its potential benefit in the treatment of infections caused by common Gram-positive pathogens.

scholarly journals Antibacterial Triterpenoids from the Bark of Sonneratia alba (Lythraceae)

2015 ◽  
Vol 10 (2) ◽  
pp. 1934578X1501000
Author(s):  
Harizon ◽  
Betry Pujiastuti ◽  
Dikdik Kurnia ◽  
Dadan Sumiarsa ◽  
Yoshihito Shiono ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Mass Spectrometric ◽  
Broth Microdilution ◽  
Mass Spectrometric Data ◽  
Spectrometric Data ◽  
Gram Positive Bacteria ◽  
Microdilution Method ◽  
Sonneratia Alba ◽  
Broth Microdilution Method

The new lupane-type triterpenoid, 3β-hydroxy-lup-9(11), 12-diene, 28-oic acid (1), along with two known lupane-type triterpenoids, lupeol (2) and lupan-3p-ol (3), were isolated from the bark of Sonnetaria alba. The structure of the new compound was elucidated on the basis of spectroscopic and mass spectrometric data analysis. Using the broth microdilution method, all compounds exhibited antibacterial activity against the Gram-positive bacteria Staphylococcus aureus ATCC 6538 and Streptococcus mutans ATCC 25175, with minimum inhibitory concentrations ranging from 15-33 to 35-55 ng/mL, respectively.

scholarly journals Chemical Composition and Antimicrobial Activity of Anthriscus nemorosa Root Essential Oil

2011 ◽  
Vol 6 (2) ◽  
pp. 1934578X1100600
Author(s):  
Milica Pavlović ◽  
Silvana Petrović ◽  
Marina Milenković ◽  
Maria Couladis ◽  
Olga Tzakou ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Essential Oil ◽  
Gram Positive Bacteria ◽  
Microdilution Method ◽  
Broth Microdilution Method ◽  
Bacillus Subtilis Atcc ◽  
Germacrene D ◽  
Main Components ◽  
Total Oil ◽  
Root Essential Oil

The essential oil obtained by hydrodistillation from the roots of Anthriscus nemorosa (Bieb.) Sprengel (Umbelliferae) was analyzed by GC and GC-MS. Among sixty-two compounds identified (representing 89.0% of the total oil), the main components were: n-nonane (12.1%), n-hexadecanol (6.9%), δ-cadinene (6.4%), β-pinene (6.0%) and germacrene D (5.4%). Furthermore, the antimicrobial activity of the oil was evaluated against the Gram-positive bacteria Staphylococcus epidermidis (ATCC 12228) and Bacillus subtilis (ATCC 6633), the Gramnegative bacterium Escherichia coli (ATCC 25922), and a yeast Candida albicans (ATCC 10259 and ATCC 24433) using the broth microdilution method.

scholarly journals Chemical Composition and Antibacterial and Cytotoxic Activities ofAllium hirtifoliumBoiss

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Salmiah Ismail ◽  
Farid Azizi Jalilian ◽  
Amir Hossein Talebpour ◽  
Mohsen Zargar ◽  
Kamyar Shameli ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Chemical Composition ◽  
Mammalian Cells ◽  
Pathogenic Bacteria ◽  
Cytotoxic Activities ◽  
Hexadecenoic Acid ◽  
Minimum Concentration ◽  
Gram Positive Bacteria ◽  
Microdilution Broth

Allium hirtifoliumBoiss. known as Persian shallot, is a spice used as a traditional medicine in Iran and, Mediterranean region. In this study, the chemical composition of the hydromethanolic extract of this plant was analyzed using GC/MS. The result showed that 9-hexadecenoic acid, 11,14-eicosadienoic acid, and n-hexadecanoic acid are the main constituents. The antibacterial activity of the shallot extract was also examined by disk diffusion and microdilution broth assays. It was demonstrated that Persian shallot hydromethanolic extract was effective against 10 different species of pathogenic bacteria including methicillin resistantStaphylococcus aureus(MRSA), methicillin sensitiveStaphylococcus aureus(MSSA),Staphylococcus aureus,Staphylococcus epidermidis,Streptococcus pneumoniae,Escherichia coli, Escherichia coliO157:H7,Salmonella typhimurium, Proteus mirabilis, andKlebsiella pneumoniae. Specifically, the minimum concentration of the extract which inhibited bacterial growth (MIC values) was 1.88 mg/mL for most of the gram-positive bacteria. This concentration was not much different from the concentration that was safe for mammalian cells (1.50 mg/mL) suggesting that the hydromethanolic extract of Persian shallot may be a safe and strong antibacterial agent.

scholarly journals Chemical Composition, and Cytotoxic, Antioxidant and Antibacterial Activities of the Essential Oil from Ginseng Leaves

2014 ◽  
Vol 9 (6) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Rui Jiang ◽  
Liwei Sun ◽  
Yanbing Wang ◽  
Jianzeng Liu ◽  
Xiaodan Liu ◽  
...  
Keyword(s):  
Essential Oil ◽  
Biological Activities ◽  
Radical Scavenging ◽  
Complex Mixture ◽  
Annexin V ◽  
Antibacterial Activities ◽  
Cytotoxic Activities ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Gram Positive Bacteria

Panax ginseng C.A.Meyer is one of the most valuable traditional Chinese medicines. In this study, the essential oil of ginseng leaves (EOGL), collected using hydrodistillation and analyzed by GC/MS, contained a complex mixture of aliphatic (69.0%), terpenoid (21.5%) and aromatic compounds (2.4%). Among 54 components identified, the major ones were palmitic acid (36.1%), β-farnesene (15.4%), linoleic acid (9.8%) and phytol (5.6%). In the cytotoxicity study, EOGL exhibited obvious cytotoxic activities against different cancer cell lines, including Hela, A549, ZR-75-1, HT-29, SGC7901 and B16 cells. Furthermore, Annexin V-FITC/PI staining assay indicated that EOGL can induce late apoptosis of ZR-75-1 cells, and the percentage of apoptotic cells increased in a concentration-dependent manner (0.9% to 5.6% and 67.4%). In addition to this, we also found that EOGL exhibited weak DPPH radical scavenging (12.0 ± 0.4 mg/mL) and ABTS radical scavenging activities (1.6 ± 0.1 mg/mL), and showed antibacterial activity against the Gram-positive bacteria, Staphylococcus aureus and Bacillus subtilis, and the Gram-negative bacterium, Escherichia coli. The data suggest that EOGL, which possesses important biological activities, especially significant anticancer activity, could be a potential medicinal resource.

scholarly journals Antibacterial Activity of the Essential Oil of Heracleum Sibiricum

2013 ◽  
Vol 8 (9) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Dragoljub L. Miladinović ◽  
Budimir S. Ilić ◽  
Tatjana M. Mihajilov-Krstev ◽  
Dejan M. Nikolić ◽  
Olga G. Cvetković ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Essential Oil ◽  
Antimicrobial Activities ◽  
Bacterial Strains ◽  
Gram Positive Bacteria ◽  
Microdilution Method ◽  
Broth Microdilution Method ◽  
Major Chemical ◽  
Total Oil ◽  
Chemical Class

The composition and antimicrobial activity of the essential oil of Heracleum sibiricum L. (Apiaceae) was studied. The aerial part of plant was hydro-distilled and chemical composition of the essential oil was analyzed by GC and GC-MS. Forty-six compounds, corresponding to 95.12% of the total oil, were identified. Esters represented the major chemical class (69.55%) while the main constituents were octyl butanoate (36.82%), hexyl butanoate (16.08%), 1-octanol (13.62%) and octyl hexanoate (8.10%). Antibacterial activity of the essential oil and reference antibiotics against nine bacterial strains was tested by the broth microdilution method. The results of the bioassays showed that essential oil had slight antimicrobial activities against all tested microorganisms (MIC and MBC values were in the range of 2431.2 to 9724.8 μg/mL). Reference antibiotics were active in concentrations between 0.5 and 16.0 μg/mL. The results confirm that Gram-positive bacteria were more susceptible to the essential oil of H. sibiricum, in comparison with Gram-negative bacteria.

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