scholarly journals Preparation, Analysis and Antibacterial Evaluation of Some New 1,3,5-Trisubstituted Pyrazole Derivatives

Author(s):  
Anupam Sharma ◽  
Alok Pal Jain ◽  
Mayank Gangwar

The goal of this study was to develop, synthesise, and characterise a novel 1,3,5-trisubstituted-2-pyrazoline derivative, as well as test its antibacterial activity. The reaction of chalcone derivatives with succinic hydrazide in the presence of pyridine yielded the 1,3,5-tri-substituted-2-pyrazolines derivatives. The IR, 1HNMR, and mass spectral analyses were used to characterise a total of 20 substances. Antibacterial activity of the compounds was tested on five Gm+Ve bacterial strains (Staphylococcus aureus, S. Faecalis, Bacillus Substilis, P. Vulgaris, and B. Pumilus) and two Gm-Ve bacterial strains (Staphylococcus aureus, S. Faecalis, Bacillus Substilis, P. Vulgaris, and B. Pumilus) and two Gm-Ve i.e. Escherichia Coli, Klebsiella Penumoniae in two different concentration i.e. 50 and 100 µg/ml by Agar-diffusion method using Cup-plate method. Standard antimicrobial drugs were Norfloxacin and Ciprofloxacin. The antibacterial activity of substances against Gm+Ve bacterial strains (Staphylococcus Aureus, Staphylococcus Faecalis, Bacillus Substilis, Pseudomonas Vulgaris, and B. Pumilus) suggested the following order of action: BR-3 >BR-2>BR-1>CL-4>BR-4>CL-3> CL-2>CL-5>CL-6>ME-3>ME-2>ME-4>ME-5>ME-6>ME-7>CL-7>CL-8>CL-1>ME-8>ME-1>ME-8>ME-1>ME-8>ME-1>ME-8>ME-1>ME-8>ME-1>ME-8>ME-1>ME-8>ME-1>ME-8>ME-1>ME-8>ME-1>ME-8>ME The chemicals of the BR-1 to BR-4 series have the most action. ME-8, CL-8, CL-7, CL-1, ME-5, ME-6, and ME-1 have light activity, whereas CL-2, CL-5, ME-4, CL-6, ME-3, ME-2, and ME-7 have moderate activity. The compounds BR-3, BR-2, BR-1, CL-4, BR-4, and CL-3 have been shown to have excellent action. The result data of antibacterial activity suggested that Cl, Br, F, and Nitro substitution at third and Fifth position may enhance the antbacterial activity of the compounds but the methyl and methoxy substitution may resulted in reduction of the activity.

2020 ◽  
Vol 2 (1) ◽  
pp. 102
Author(s):  
Yanu Andhiarto ◽  
Rina Andayani ◽  
Nur Hidayatul Ilmiyah

Skin infections most often found in developing countries, especially in the tropics, are purulent skin inflammation (pyoderma), the main cause of Staphylococcus aureus. The increasing number of cases of bacteria that are resistant to antibacterial can encourage the extraction of sources of antibacterial drugs from natural ingredients. One of the plants that is thought to have the antibacterial activity of Staphylococcus aureus is the Neem plant. In this study an antibacterial activity test was carried out with the well diffusion method from 96% ethanol extract of Mimba leaves extracted by percolation method. Previously 96% ethanol extract from Mimba leaves had been identified by secondary metabolites by phytochemical screening and standardized extract testing. Standarization using non-specific parameters (moisture content, ash content and drying losses) found that 96% ethanol extract of Mimba leaves entered a range of standard parameters and in phytochemical screening tests obtained 96% ethanol extract of Mimba leaves containing alcaloid, saponins, tannins, steroids / terpenoids and flavonoids. The results of the study on the antibacterial activity test showed a concentration of 75% ethanol extract of 96% Mimba leaves classified as having strong activity, at a concentration of 50% and 25% classified as having moderate activity. Based on this study it can be concluded that the three concentrations of 96% ethanol extract of Mimba leaves were able to inhibit the growth of Staphylococcus aureus bacteria.


2015 ◽  
Vol 17 (4 suppl 2) ◽  
pp. 922-927 ◽  
Author(s):  
A. BURGOS ◽  
J. BARUA ◽  
M.E. FLORES-GIUBI ◽  
D. BAZAN ◽  
E. FERRO ◽  
...  

ABSTRACT The antibacterial activity of the alkaloid extract from the leaves of Croton bonplandianum Baill. and its main compounds, sparsiflorine and crotsparine, was tested against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa by the resazurin microtitre-plate method. Pure compounds were identified by spectroscopic techniques, mainly 1D and 2D NMR. The alkaloid extract showed activity particularly against the S. aureus and P. aeruginosa. Regarding the pure compounds, the crotsparine was inactive against the microorganisms assayed, whereas the sparsiflorine indicated a moderate activity similar to the alkaloid extract. The Pseudomonas aeruginosa was the most sensitive of the tested microorganisms with MIC of 0.141 mg/mL. The results suggest that the activity of the extract may be credited mainly to the presence of the sparsiflorine. Although the activity of the sparsiflorine does not get close to the antimicrobial drugs in clinical use, it still could be a lead compound for the development of new antibacterial substances.


2016 ◽  
Vol 60 (1) ◽  
pp. 5-18 ◽  
Author(s):  
Lia M. Junie ◽  
Mihaela L. Vică ◽  
Mirel Glevitzky ◽  
Horea V. Matei

AbstractThe first aim of the study was to compare the antibacterial activity of several types of honey of different origins, against some bacterial resistant strains. The strains had been isolated from patients. The second aim was to discover the correlations between the antibacterial character of honey and the physico-chemical properties of the honey. Ten honey samples (polyfloral, linden, acacia, manna, and sunflower) from the centre of Romania were tested to determine their antibacterial properties against the following bacterial species: Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus, Staphylococcus epidermidis, Salmonella enterica serovar Typhimurium, Bacillus cereus, Bacillus subtilis, and Listeria monocytogenes. Bacterial cultures in nutrient broth and the culture medium Mueller-Hinton agar were used. The susceptibility to antibiotics was performed using the disk diffusion method. All honey samples showed antibacterial activity on the isolated bacterial strains, in particular polyfloral (inhibition zone 13-21 mm in diameter) - because it is the source of several plants, and manna (inhibition zone 13-19.5 mm in diameter), and sunflower (inhibition zone 14-18.5 mm in diameter). Pure honey has a significant antibacterial activity against some bacteria which are resistant to antibiotics. Bacterial strains differed in their sensitivity to honeys. Pseudomonas aeruginosa and Staphylococcus aureus were the most sensitive. The present study revealed that honey antibacterial activity depends on the origin of the honey. We also found that there was a significant correlation between antibacterial activity of honeys and the colour of the honey but not between acidity and pH. The statistical analysis showed that the honey type influences the antibacterial activity (diameter of the bacterial strains inhibition zones).


2021 ◽  
Vol 5 (4) ◽  
pp. 375-380
Author(s):  
Ayu Nala El Muna Haerussana ◽  
Wulan Putri Dwiastuti ◽  
Cindi Arwan Sukowati

Indonesia has a high diversity of potential medicinal plants, which are the second-largest number of indigenous medicinal plants in the world. Syzygium polyanthum, known as Indonesian Bay Leaf or Salam, easily found, widely used in Indonesia as a spice in cooking and traditional medicine. Salam contains secondary metabolites such as flavonoids, alkaloids, tannins, essential oils, sesquiterpenes, triterpenes, phenols, steroids, and saponins. Staphylococcus aureus and Staphylococcus epidermidis are the main bacteria that cause commensal infection and the most common nosocomial infections. This study aims to know the antibacterial activity of the Salam ethanolic extract against Staphylococcus aureusand Staphylococcus epidermidis bacteria. Salam leaves were extracted by 70% ethanol in the maceration method. Antibacterial activity was conducted by the disk diffusion method. The extract exhibits moderate activity (10.51±0.3 mm) at 75% of concentration and low activity (3.69±0.4 mm) at 100% of concentration against Staphylococcus aureus and Staphylococcus epidermidis respectively. The test showed that salam leaves extract had antibacterial activity against Staphylococcus aureus and Staphylococcus epidermidis.


2019 ◽  
Vol 9 (1-s) ◽  
pp. 98-100 ◽  
Author(s):  
B.C. Joshi ◽  
Vinod Kumar ◽  
Bhuwan Chandra ◽  
N.D. Kandpal

Objective: Among natural products, essential oils and their contituents represent a structurally diverse group of organic compounds with significant antibacterial activity. This  study  is  oriented  to  assess  the  therapeutic  potential  of  plant constituents as new antimicrobial drugs. Methods: Aerial parts of Senecio graciliflorus was steam distilled and analysed by GC and GC-MS for the volatile constituents. Essential oil was studied for their antibacterial activity against Gram-positive and Gram-negative bacteria using agar well diffusion method. Results: The results revealed that α-pinene and α-thujene are the major constituents of S. graciliflorus oil. In vitro studies showed significant antimicrobial activity against bacterial strains. Conclusion: This study demonstrated that the oil significantly inhibits the growth of baceria. S. graciliflorus would be another alternative for developing new pharmaceuticals for prevention bacterial diseases and provide a direction for the study of naturally derived drugs. Keywords: Asteraceae, Senecio graciliflorus, Essential oil, α-Pinene, Antibacterial activity.


Author(s):  
Kyoung- Sun Seo ◽  
Seong Woo Jin ◽  
Seongkyu Choi ◽  
Kyeong Won Yun

The antibacterial activity of three Cupressaceae plants (Thujaoccidentalis,ThujaorientalisandChamaecyparisobtusa) was tested against three bacteria using the agar diffusion method. The ether and ethylacetate fraction of crude methanol extract from the three plants showed potent antibacterial activity against the tested microorganisms. The result showed that Staphylococcus aureus revealed the most sensitivity among the tested bacteria. Thujaoccidentalisether fraction and Thujaorientalis hexane fraction exhibited the highest antibacterial activity against Staphylococcus aureus. E. coli was shown the highest MIC values compared to the other two tested bacteria, which indicates the lowest antibacterial activity against the bacterium. This study promises an interesting future for designing a potentially active antibacterial agent from the three Cupressaceae plants.


2015 ◽  
Vol 2015 ◽  
pp. 1-6 ◽  
Author(s):  
Mohammed El Fal ◽  
Youssef Ramli ◽  
Abdelfettah Zerzouf ◽  
Ahmed Talbaoui ◽  
Youssef Bakri ◽  
...  

New heterocyclic compounds spiroderivatives of allopurinol of biological interest were prepared from allopurinol via thionation and 1,3-dipolar cycloaddition and were produced in high to excellent yields. These compounds were characterized on the basis of spectral and spectroscopic data (1H NMR,13C, IR, and MS). The antibacterial activity of the synthesized products was studied using bacterial strains:Staphylococcus aureus,Enterococcus faecalis,Escherichia coli, andPseudomonas aeruginosa. Compounds having an ethyl group showed the best activity with MIC value of 31.25 µg/mL againstStaphylococcus aureusandStreptococcus fasciens.


2011 ◽  
Vol 76 (9) ◽  
pp. 1199-1206 ◽  
Author(s):  
Raju Chaudhari ◽  
Sahebrao Rindhe

Herein the synthesis of a series of novel 8-(1- alkyl/alkylsulphonyl/alkoxycarbonyl-benzimidazol-2-ylmethoxy)-5- chloroquinoline derivatives is reported. These derivatives were prepared by the condensation of o-phenylenediamine with [(5-chloroquinolin-8- yl)oxy]acetic acid, followed by substitution at nitrogen with different electrophilic reagents in presence of an appropriate base to give a series of nitrogen heterocycles containing the benzimidazole and quinoline nuclei. The structures of the compounds were confirmed based on 1H-NMR, 13CNMR, IR and mass spectral data. Almost all the compounds exhibited promising antibacterial activity against Salmonella typhimurium and Staphylococcus aureus. Some of the compounds showed good antifungal activities against Aspergillus niger but the antifungal activities against Candida albicans were disappointing.


2017 ◽  
Vol 2 (2) ◽  
pp. 239
Author(s):  
Ratih Dyah Pertiwi ◽  
Joni Kristanto ◽  
Graha Ayu Praptiwi

One of plants used by Indonesian people as a traditional medicine is saga plant (Abrus precatorius L.). This plant has medicinal properties as medication for thrush, cough and laryngitis. Chemical constituents contained in sage leaves which work as antibacterial are flavonoid and saponin. This study aims to determine the optimal concentration of saga leaves extract which can be formulated in a gel dosage form with qualified physical evaluation and has antibacterial activity against Staphylococcus aureus. Saga leaves extract is prepared by maceration method using ethanol 70% as solvent, and then the extract obtained is preliminarily tested to see its antibacterial activity against Staphylococcus aureus with agar diffusion method. Gel formulation for thrush is made with dispersion method in three formulas with variants of active substance concentration that is FI (1%), FII (3%) and FIII (5%). Gel preparation antibacterial activity test is conducted with agar diffusion method as a plate cylinder. Based on this research, it was found that the extract of saga leaves which is positively made is efficacious as antibacterial and can be formulated into a gel preparation for thrush with optimal concentration in F III (5%), this is indicated by widest diameter of the inhibition area against Staphylococus aureus bacteria


Author(s):  
Selvarani Murugan

Objective: Resistance to antibacterial agents by pathogenic bacteria has emerged in recent years and is a major challenge for the healthcare industry. Copper nanoparticles (CuNPs) are known to be one of the multifunctional inorganic nanoparticles with effective antibacterial activity. Hence the present investigation has been focused on synthesizing and evaluating the bactericidal effect of copper nanoparticles.Methods: CuNPs were synthesized by reducing the aqueous solution of copper sulfate with sodium borohydride. The synthesized particles were characterized by x-ray diffractogram (XRD), scanning electron microscopy (SEM) and energy dispersive spectroscopy (EDS) techniques to analyze size, morphology and quantitative information respectively. The antibacterial activity of CuNPs was examined by agar well diffusion method. Synergistic effect of CuNPs with broad-spectrum antibiotics was determined by the agar disc diffusion method.Results: Color change of reaction mixture from blue to dark brown indicated the formation of CuNPs. SEM image clearly demonstrated that the synthesized particles were spherical in shape and its size was found to be 17.85 nm. EDS report confirmed the presence of elemental copper in the resultant nanoparticles and its accounts for major proportion (96%) of the mass of nanoparticles. Bacterial effect of CuNPs revealed that Pseudomonas aeruginosa showed the highest antibacterial sensitivity (16.00±1.63 mm), whereas least susceptibility (9.67±0.47 mm) was noticed against Staphylococcus aureus. An enhanced antibacterial activity of commercial antibiotics was also noticed when it combined with CuNPS. A minimum zone of inhibition was increased from 0.67±0.47 mm to 10.66±0.24 mm when the nanoparticles and antibiotics were given together.Conclusion: It was observed that copper nanoparticles exhibited profound activity against all the tested bacterial strains which shows that CuNPs may serve as a better option for use in medicine in the future.


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