scholarly journals Synthesis of N'-(7-Chloroquinolin-4-yl)-6-Methyl-2-Oxo-4-Phenyl-1,2,3,4-Tetrahydropyrimidine-5-Carbohydrazide Derivatives as Potent Antibacterial Agents

2015 ◽  
Vol 56 ◽  
pp. 82-90 ◽  
Author(s):  
Manoj N. Bhoi ◽  
Mayuri A. Borad ◽  
Edwin A. Pithawala ◽  
Shweta Modi ◽  
Hitesh D. Patel
Keyword(s):  
Elemental Analysis ◽  
Bacterial Strain ◽  
Antibacterial Agents ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative ◽  
Ft Ir

Some novel N'-(7-chloroquinolin-4-yl)-6-methyl-2-oxo-4-phenyl-1,2,3,4-tetrahydropyrimidine-5-carbohydrazide derivatives were synthesized via three step reactions by convectional method. The structures of all the compounds have been confirmed by FT-IR, NMR, and MASS and by elemental analysis. We have been evaluated it inhibition capacity for various gram positive and gram negative bacterial strain. All compounds were found to be good to excellent active against all four bacterial strains.

scholarly journals Synthesis and Antimicrobial Assessment of Some New 2-(Thiazol-5-yl)-1,3,4-oxadiazoles

2019 ◽  
Vol 70 (6) ◽  
pp. 1996-1999
Author(s):  
Catalin Araniciu ◽  
Smaranda Dafina Oniga ◽  
Cristina Ioana Stoica ◽  
Mariana Carmen Chifiriuc ◽  
Marcela Popa ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Physicochemical Characterization ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative ◽  
Fungal Strains ◽  
New Compounds

Considering the promising antimicrobial activity of compounds bearing the thiazole or the oxadiazole rings in their structures, we set out to obtain new antimicrobial molecules bearing the 2-(thiazol-5-yl)-1,3,4-oxadiazole schaffold. The structures of the 8 new compounds obtained was confirmed by physicochemical characterization including: 1H-NMR, MS and elemental analysis. Antimicrobial activity was investigated against 5 Gram-positive bacterial strains, 2 Gram-negative bacterial strains and 2 fungal strains. The newly synthesized compounds showed modest antimicrobial activity.

scholarly journals Synthesis, Characterization and Antibacterial Activity Evaluation of New Indole-Based Derivatives

2020 ◽  
Vol 29 (1) ◽  
pp. 207-2015
Author(s):  
Ahmed T. Sulaiman ◽  
Susan W. Sarsam
Keyword(s):  
Antibacterial Agents ◽  
Glacial Acetic Acid ◽  
Diffusion Method ◽  
Moderate Activity ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Different Types ◽  
Ft Ir

A new series of N-acyl hydrazones (4a-g) derived from indole-3-propionic acid (IPA) were synthesized. These N-acyl hydrazones were prepared by the reaction of 3-(1H-indol-3-yl) propane hydrazide and aldehyde in the existence of glacial acetic acid as a catalyst. 1HNMR and FT-IR analyses were used to identify the synthesized compounds and they were in vitro evaluated as antibacterial agents against six different types of microorganisms by using well diffusion method. All the tested N-acyl hydrazones (4a-g) displayed moderate activity against the Gram-negative E.coli, comparable to that of Amoxicillin. Some of the tested N-acyl hydrazones also exhibited intermediate activity against some of the examined Gram-positive and Gram-negative bacteria. While no activity was exhibited by any of the examined compounds against the Gram-positive S. aureus.

Synthesis and Biological Evaluation of a New Schiff Base and its Cu(II) Complex

2017 ◽  
Vol 68 (3) ◽  
pp. 586-588
Author(s):  
Gladiola Tantaru ◽  
Antonia Poiata ◽  
Nela Bibire ◽  
Alina Diana Panainte ◽  
Mihai Apostu ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Schiff Base ◽  
Elemental Analysis ◽  
Schiff Base Ligand ◽  
Biological Evaluation ◽  
Gram Negative Bacteria ◽  
Bacterial Strains ◽  
Gram Negative ◽  
Ft Ir ◽  
Synthesis And Biological Evaluation

A new Schiff base ligand, N-hydroxy-N�-salicylidene-urea was synthesized through the condensation of salicylaldehyde with hydroxyurea. The copper(II) complex of the Schiff base has been also obtained. Their structure has been proven using spectral methods such as UV-Vis, FT-IR, 1H-NMR and elemental analysis. The antimicrobial activity of the copper(II) complex was evaluated through comparison to the activity of the Schiff base on various bacterial strains. All tested compounds were very active against both gram-positive and gram-negative bacteria.

scholarly journals Structure-Antibacterial Activity Relationships Of N-Substituted-(D-/L-Alaninyl) 1H-1,2,3-Triazolylmethyl Oxazolidinones

2018 ◽  
Author(s):  
Oludotun Phillips ◽  
Edet Ekpenyong Udo ◽  
Roselyn Jennifer D’silva
Keyword(s):  
Antibacterial Activity ◽  
Antibacterial Agents ◽  
Bacterial Resistance ◽  
Clinical Usefulness ◽  
Antibacterial Resistance ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Resistance Development ◽  
Antibacterial Drugs ◽  
Gram Negative

Bacterial resistance towards existing class of antibacterial drugs continues to increase posing significant threat to clinical usefulness of these drugs. This increasing and alarming rates of antibacterial resistance development and the decline in the number of new antibacterial drugs approval continue to serve as major impetus for research into discovery and development of new antibacterial agents. We synthesized a series D-/L-alaninyl substituted triazolyl oxazolidinone derivatives and evaluated their antibacterial activity against selected standard Gram-positive and Gram-negative bacterial strains. Overall, the compounds showed moderate to strong antibacterial activity. Compounds 9d and 10d (D- and L-alaninyl derivatives bearing 3,5-dinitrobenzoyl substituent), 10e (D-alaninyl derivative bearing 5-nitrofurancarbonyl group) and 9f and 10f (D- and L-alaninyl derivatives bearing 5-nitrothiophene carbonyl moiety) demonstrated antibacterial activity (MIC:2 g/mL) against S. aureus, S. epidermidis, E. faecalis and M. catarrhalis standard bacterial strains. No significant differences were noticeable between the antibacterial activity of the D- and L-alaninyl derivatives as a result of the stereochemistry of the compounds.

scholarly journals Synthesis, Characterization and Antibacterial Studies of (3,3-Dimethyl-7-oxo-6-(2-phenylacetamido)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid-Cr (III) Complex

2020 ◽  
Vol 41 (1) ◽  
pp. 1-7
Author(s):  
Ifeanyi Edozie Otuokere ◽  
Unwanaobong Friday Robert
Keyword(s):  
Antibacterial Activity ◽  
Metal Complex ◽  
Metal Ion ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative ◽  
Spectroscopic Result ◽  
Trigonal Bipyramidal ◽  
Ft Ir

Benzylpenicillin, also known as (3,3-Dimethyl-7-oxo-6-(2-phenylacetamido)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic, is a common bactericidal antibiotic of the betalactamin family which is mostly used to treat infections caused by gram-positive bacterial strains and few gram-negative bacterial strains. Cr (III) complex of benzylpenicillin was synthesized by the reaction of benzylpenicillin with CrCl3.6H2O. The structure of the complex was confirmed through elemental analysis, electrical conductivity, FT-IR, electronic spectra, 1H-NMR, and 13C-NMR spectroscopic methods. The physical properties such as solubility, color and melting point were also determined for both the ligand and the complex. The complex has a deep green color. Both the ligand and the complex are ionic (236.0 and 126.0 Sm2.mol-1). From the spectroscopic result, the ligand behaved as a pentadentate ligand coordinating to the metal ion through OH, NH, C=O of amide, carboxylate& β-lactam. A trigonal bipyramidal geometry has been proposed for the metal complex. The prepared complex was evaluated in vitro for its antibacterial activity against some pathogenic gram-positive (Staphylococcus aureus, Bacillus substilis, Bacillus cereus, and Enterococcus faecalis) and gram-negative bacteria (Escherichia coli, Enterobacter cloacae, Pneumonia aeruginosa and Campylobacter fetus). The metal complex showed enhanced antibacterial activity as compared to the uncomplexed ligand.

scholarly journals Synthesis, Characterization and Biological Activity Of 1, 4-Dihydropyrimido [1,2-A] Benzimidazole

2021 ◽  
pp. 267-274
Author(s):  
Vaishnavi. P. Gilava ◽  
Dr. Praful. K. Patel
Keyword(s):  
Antimicrobial Activity ◽  
Biological Activity ◽  
Elemental Analysis ◽  
Direct Synthesis ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative

An effectual direct synthesis of 1,4-dihydropyrimido[1,2-a]benzimidazole (C-01 to C-10) was developed from 1H-benzo[d]imidazol-2-amine, 4-(benzyloxy)-3-methoxybenzaldehyde, N-(substituted phenyl)-3-oxobutanamide by adding few drop of DMF and in presence of conc.HCL. The product was obtained after about 5 hours of heating in refluxing condition. The synthesized compounds were characterized by different spectral and elemental analysis. Some of the obtained compounds showed a promising antimicrobial activity on screening against Gram-positive and Gram-negative bacterial strains.

Antimicrobial Activity of Iron-Halide Complexes Against Gram-Positive and Gram-Negative Bacteria

2020 ◽  
Author(s):  
Nusrat Abedin ◽  
Abdullah Hamed A Alshehri ◽  
Ali M A Almughrbi ◽  
Olivia Moore ◽  
Sheikh Alyza ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Resistance ◽  
Extracellular Dna ◽  
Antibiofilm Activity ◽  
Gram Negative Bacteria ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative ◽  
Antimicrobial Substances ◽  
Mammalian Cell Lines

Antimicrobial resistance (AMR) has become one of the more serious threats to the global health. The emergence of bacteria resistant to antimicrobial substances decreases the potencies of current antibiotics. Consequently, there is an urgent and growing need for the developing of new classes of antibiotics. Three prepared novel iron complexes have a broad-spectrum antimicrobial activity with minimum bactericidal concentration (MBC) values ranging from 3.5 to 10 mM and 3.5 to 40 mM against Gram-positive and Gram-negative bacteria with antimicrobial resistance phenotype, respectively. Time-kill studies and quantification of the extracellular DNA confirmed the bacteriolytic mode of action of the iron-halide compounds. Additionally, the novel complexes showed significant antibiofilm activity against the tested pathogenic bacterial strains at concentrations lower than the MBC. The cytotoxic effect of the complexes on different mammalian cell lines show sub-cytotoxic values at concentrations lower than the minimum bactericidal concentrations.

scholarly journals Ultrasonic Irradiation: Synthesis, Characterization, and Preliminary Antimicrobial Activity of Novel Series of 4,6-Disubstituted-1,3,5-triazine Containing Hydrazone Derivatives

2016 ◽  
Vol 2016 ◽  
pp. 1-9 ◽  
Author(s):  
Hessa H. Al-Rasheed ◽  
Monirah Al Alshaikh ◽  
Jamal M. Khaled ◽  
Naiyf S. Alharbi ◽  
Ayman El-Faham
Keyword(s):  
Antimicrobial Activity ◽  
Ultrasonic Irradiation ◽  
New Products ◽  
Conventional Heating ◽  
Pyridine Derivative ◽  
Gram Negative Bacteria ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative ◽  
Antimicrobial And Antifungal Activities

Novel series of 4,6-disubstituted-1,3,5-triazines containing hydrazone derivatives were synthesized employing ultrasonic irradiation and conventional heating. The ultrasonication gave the target products in higher yields and purity in shorter reaction time compared with the conventional method. IR, NMR (H 1 and C 13), elemental analysis, and LC-MS confirmed the structures of the new products. The antimicrobial and antifungal activities were evaluated for all the prepared compounds against some selected Gram-positive and Gram-negative bacterial strains. The results showed that only two compounds 7i (pyridine derivative) and 7k (4-chlorobenzaldehyde derivative) displayed biological activity against some Gram-positive and Gram-negative bacteria, while the rest of the tested compounds did not display any antifungal activity.

scholarly journals Microwave Assisted Synthesis and Antimicrobial Evaluation of Schiff Bases of Indole-3-aldehyde

2011 ◽  
Vol 8 (1) ◽  
pp. 305-311 ◽  
Author(s):  
Priyanka Kamaria ◽  
N. Kawathekar ◽  
Prerna Chaturvedi
Keyword(s):  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Microwave Assisted Synthesis ◽  
Bacterial Strains ◽  
Mass Spectral Analysis ◽  
Gram Positive ◽  
Gram Negative ◽  
Mass Spectral ◽  
Microwave Assisted ◽  
Antimicrobial Evaluation

In order to develop new antimicrobial agents, a series of Schiff bases of indole-3-aldehyde were synthesized by microwave assisted synthesis by takingDMFas solvent and evaluated for their antimicrobial activity. All the synthesized compounds were characterized byIR,1HNMRand mass spectral analysis. All compounds were tested against five gram positive and five gram negative bacterial strains and one fungal strain. All compounds exhibited better activity against gram positive strains than against gram negative strains and the compounds were found more active againstS.aureusandB.subtilis.

scholarly journals Anticancer and Antimicrobial Activity Evaluation of Cowpea-Porous-Starch-Formulated Silver Nanoparticles

2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Shiara Ramdath ◽  
John Mellem ◽  
Londiwe Simphiwe Mbatha
Keyword(s):  
Antimicrobial Activity ◽  
Silver Nanoparticles ◽  
Cell Viability ◽  
High Dose ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative ◽  
Anticancer Drug Delivery ◽  
Ic50 Values ◽  
Biosynthesized Agnps

Health issues involving inadequate treatment of diseases such as cancer and microbial infections continue to be the subject of much ongoing recent research. Biosynthesized silver nanoparticles (AgNPs) were characterized using Transmission Electron Microscopy (TEM), Zeta Sizer, Ultraviolet (UV), and Fourier Transform Infrared (FTIR) spectroscopy. Their antimicrobial activity was evaluated on selected Gram-positive and Gram-negative bacterial strains, using the disc diffusion and broth dilution assays. Cell viability profiles were evaluated using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) and apoptosis studies on selected human noncancer and cancer cells. The biosynthesized AgNPs were evaluated to be spherical clusters, with sizes between 40 and 70 nm. The absorption peak at 423 nm and the presence of polyphenols confirmed the synthesis and stabilization of these tested AgNPs. The AgNPs showed a good stability of −23.9 ± 1.02 mV. Good antimicrobial activity (6.0–18.0 mm) was seen on all tested bacteria at a minimum inhibitory concentration (MIC) ranging from 5 to 16 μg/ml, with the highest activity seen against Gram-negative Escherichia coli (18 ± 0.5 mm), and the lowest activity was seen against Gram-positive Listeria monocytogenes (6.0 ± 0.4 mm) after treatment with the AgNPs. These NPs showed a concentration-dependent and cell-specific cytotoxicity with low IC50 values (41.7, 56.3, and 63.8 μg/ml). The NPs were well tolerated by tested cells as indicated by a more than 50% cell viability at the high dose tested and low apoptotic indices (<0.2). These findings indicated that these biosynthesized AgNPs showed great potential as effective antibacterial agents and anticancer drug delivery modalities.

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