scholarly journals Synthesis and Antibacterial Activity of Chalcones and Pyrimidine-2-ones

2005 ◽  
Vol 2 (2) ◽  
pp. 109-112
Author(s):  
A. K. Parekh ◽  
K. K. Desai

Some new chalcones have been prepared by Claisen-schmidt condensation of ketone and different aromatic aldehydes. These chalcones on condensation with urea in presence of acid gave Pyrimidine-2-ones. The synthesized compounds have been characterized by elemental analysis, IR and1H NMR spectral data. They have been screened for their antibacterial activity against Gram positive bacteria B. subtillis & S. aureus and Gram negative bacteria E. coli & S. typhi.

2007 ◽  
Vol 72 (5) ◽  
pp. 443-449 ◽  
Author(s):  
Tejaskumar Shah ◽  
Vikas Desai

A series of 3-[3-(2,4-dichloro-5-fluorophenyl)-5-(2-furyl)-4,5-dihydro-1H-pyrazol- 1-yl]-5-(substituted phenyl/2-thienyl)isoxazolines (4a-j) were prepared. The structures of the isoxazoline derivatives were confirmed on the bases of elemental analysis and spectral data. The compounds were screened for their in vitro antibacterial activity using gram-positive bacteria and gram-negative bacteria.


2012 ◽  
Vol 9 (1) ◽  
pp. 481-486
Author(s):  
K. Anuradha ◽  
R. Rajavel

Novel Cu(II),Ni(II) and VO(II) complexes are synthesized with N1,N4-bis(2-aminobenzylidene)benzene-1,4-diamine (L). Complexes were characterized by elemental analysis, molar conductance, IR, UV and EPR. Spectral studies reveals a square planner geomentry for Cu(II), Ni(II) complexes and square pyramidal for VO(II) complex. The ligand and its complexes were also evaluated against the growth of gram positive bacteria and gram negative bacteria.


2019 ◽  
Vol 18 (5) ◽  
pp. 1147-1155 ◽  
Author(s):  
Rehan Khan ◽  
Melis Özkan ◽  
Aisan Khaligh ◽  
Dönüs Tuncel

Water-dispersible glycosylated poly(2,5′-thienylene)porphyrin-based nanoparticles have the ability to generate singlet oxygen in high yields and exhibit light-triggered antibacterial activity against Gram negative bacteria, E. coli as well as Gram positive bacteria, B. subtilis.


Author(s):  
Elaf Ayad Kadhem ◽  
Miaad Hamzah Zghair ◽  
Sarah , Hussam H. Tizkam, Shoeb Alahmad Salih Mahdi ◽  
Hussam H. Tizkam ◽  
Shoeb Alahmad

magnesium oxide nanoparticles (MgO NPs) were prepared by simple wet chemical method using different calcination temperatures. The prepared NPs were characterized by Electrostatic Discharge (ESD), Scanning Electron Microscope (SEM) and X-ray Diffraction (XRD). It demonstrates sharp intensive peak with the increase of crystallinty and increase of the size with varying morphologies with respect to increase of calcination temperature. Antibacterial studies were done on gram negative bacteria (E.coli) and gram positive bacteria (S.aureus) by agar disc diffusion method. The zones of inhibitions were found larger for gram positive bacteria than gram negative bacteria, this mean, antibacterial MgO NPs activity more active on gram positive bacteria than gram negative bacteria because of the structural differences. It was found that antibacterial activity of MgO NPs was found it has directly proportional with their concentration.


2020 ◽  
Vol 16 (4) ◽  
pp. 481-488
Author(s):  
Heli Sanghvi ◽  
Satyendra Mishra

Background: Curcumin, one of the most important pharmacologically significant natural products, has gained significant consideration among scientists for decades since its multipharmacological activities. 1, 3-Dicarbonyl moiety of curcumin was found to be accountable for the rapid degradation of curcumin molecule. The aim of present work is to replace 1, 3-dicarbonyl moiety of curcumin by pyrazole and phenylpyrazole derivatives with a view to improving its stability and to investigate the role of substitution in N-phenylpyrazole curcumin on its antibacterial activity against both Gram-positive as well as Gram-negative bacteria. Methods: Pyrazole derivatives of curcumin were prepared by heating curcumin with phenyhydrazine/ substituted phenyhydrazine derivatives in AcOH. The residue was purified by silica gel column chromatography. Structures of purified compounds were confirmed by 1H NMR and Mass spectroscopy. The synthesized compounds were evaluated for their antibacterial activity by the microdilution broth susceptibility test method against gram positive (S. aureus) and gram negative (E. coli). Results: Effects of substitution in N-phenylpyrazole curcumin derivatives against S. aureus and E. coli were studied. The most active N-(3-Nitrophenylpyrazole) curcumin (12) exhibits twenty-fold more potency against S. aureus (MIC: 10μg/mL)) and N-(2-Fluoroophenylpyrazole) curcumin (5) fivefold more potency against E. coli (MIC; 50 μg/mL) than N-phenylpyrazole curcumin (4). Whereas, a remarkable decline in anti-bacterial activity against S. aureus and E. coli was observed when electron donating groups were incorporated in N-phenylpyrazole curcumin (4). Comparative studies of synthesized compounds suggest the effects of electron withdrawing and electron donating groups on unsubstituted phenylpyrazole curcumin (4). Conclusion: The structure-activity relationship (SAR) results indicated that the electron withdrawing and electron donating at N-phenylpyrazole curcumin played key roles for their bacterial inhibitory effects. The results of the antibacterial evaluation showed that the synthesized pyrazole derivatives of curcumin displayed moderate to very high activity in S. aureus. In conclusion, the series of novel curcumin derivatives were designed, synthesized and tested for their antibacterial activities against S. aureus and E. coli. Among them, N-(3-Nitrophenylpyrazole curcumin; 12) was most active against S. aureus (Gram-positive) and N-(2-Fluoroophenylpyrazole) curcumin (5) against E. coli (Gram-negative) bacteria.


2012 ◽  
Vol 7 (5) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Alexis Peña ◽  
Luis Rojas ◽  
Rosa Aparicio ◽  
Libia Alarcón ◽  
José Gregorio Baptista ◽  
...  

The essential oil of the leaves of Espeletia nana Cuatrec, obtained by hydrodistillation, was analyzed by GC-MS, which allowed the identification of 24 components, which made up 99.9% of the oil. The most abundant compounds were α-pinene (38.1%), β-pinene (17.2%), myrcene (15.0%), spathulenol (4.2%), bicyclogermacrene (4.0%), α-zingiberene (4.0%), and γhimachalene (3.7%). Antibacterial activity was tested against Gram-positive and Gram-negative bacteria using the agar disk diffusion method. Activity was observed only against Gram-positive bacteria. MIC values were determined for Staphylococcus aureus ATCC 25923(200 μg/mL) and Enterococcus faecalis ATCC 29212 (600 μg/mL).


2019 ◽  
Vol 43 (9-10) ◽  
pp. 307-312
Author(s):  
Amira A El-Sayed ◽  
Saad R Atta-Allah ◽  
Magdy M Hemdan

Convenient syntheses of quinazoline, benzothiazole, thiadiazole, imidazole, and thiourea derivatives starting from 3-(thiophen-2-yl)prop-2-enoyl isothiocyanate are described. The structures of the synthesized compounds are confirmed from their microanalytical and spectral data. Some of the products are examined for their antibacterial activity against Gram-positive and Gram-negative bacteria and fungi.


2020 ◽  
Vol 840 ◽  
pp. 265-269
Author(s):  
Nurjanah Nurjanah ◽  
Endang Saepudin

Curcumin, a diarylheptanoids compound which isolated primary from Curcuma longa, exhibits a variety of exciting biological activities, including as an antibacterial agent. In the present study, a sulfanilamide-contained curcumin compound was synthesized and characterized to investigate the antibacterial activity against gram-positive bacteria S. aureus, B. subtilis and gram-negative bacteria E. coli. The characterization of the synthesized compound was determined by analysing peak absorbance, functional group, and molecular weight using mass spectroscopy, UV/Vis and FTIR spectrophotometry. Curcumin-sulfanilamide compound exhibited the best antibacterial activity against gram-negative bacteria compared to curcumin and the curcumin-derived compound containing isoxazole with inhibitory zone of 11 mm.


2013 ◽  
Vol 2 (1) ◽  
pp. 147-152 ◽  
Author(s):  
AM Bukar ◽  
MA Isa ◽  
HS Bello ◽  
AS Abdullahi

The phytochemical screening and antibacterial activity of ethanolic and Methanolic leaves extract of Vernonia amygdalina against five clinical isolates (Staphylococcus aureus, E. coli, Pseudomonas species, Salmonella species and Proteus species) was determined using standard method of analysis. The results of the antibacterial activity of ethanol, methanol and aqueous extract of leaves of V. amygdalina have diameters ranging between 0.4 to 10mm. The plant extracts from the plants had profound activities against gram-positive than gram negative bacteria. From the above studies, it has clearly indicated that V. amygdalina extract may represent new sources of antibacterial drug, if the phytoactive components are purified and proper dosage are determined for administration. International Journal of Environment, Volume-2, Issue-1, Sep-Nov 2013, Pages 147-152 DOI: http://dx.doi.org/10.3126/ije.v2i1.9217


2018 ◽  
Vol 86 (4) ◽  
pp. 48 ◽  
Author(s):  
Rubén Vilcacundo ◽  
Pilar Méndez ◽  
Walter Reyes ◽  
Herman Romero ◽  
Adelita Pinto ◽  
...  

The aim of this study was to increase the antibacterial spectrum of modified hen egg white lysozyme (HEWL) with thermal and chemical treatments against Gram-negative bacteria. The antibacterial activity of heat-denatured HEWL and chemical denatured HEWL against Gram-negative and Gram-positive bacteria was evaluated in 15 h of incubation tests. HEWL was denatured by heating at pH 6.0 and pH 7.0 and chemical denaturing was carried out for 1.0, 1.5, 2.0, and 4.0 h with DL-Dithiothreitol (DTT). HEWL modified by thermal and chemical treatments was characterized using the sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) electrophoresis method. Heat-denatured HEWL lytic activity against Micrococcus lysodeikticus lessened with increasing temperature and time of incubation with the chemical agent (DTT). The loss of lytic activity in modified HEWL suggests that the mechanism of action of the antibacterial activity is not dependent on the lytic activity. Thermal and chemical treatments of HEWL enabled the production of oligoforms and increased antibacterial activity over a wider spectrum. Heat-denatured HEWL at pH 6.0 and chemically-denatured HEWL increased the HEWL antibacterial spectrum against Gram-negative bacteria (Escherichia coli ATCC 25922). HEWL at 120 °C and pH 6.0 (1.0 mg/mL) inhibited 78.20% of the growth of E. coli. HEWL/DTT treatment for 4.0 h (1.0 mg/mL) inhibited 68.75% of the growth E. coli. Heat-denatured HEWL at pH 6.0 and pH 7.0 and chemically-denatured HEWL (1.0, 1.5, 2.0, and 4.0 h with DTT) were active against Gram-positive bacteria (Staphylococcus carnosus CECT 4491T). Heat-denatured and chemical-denatured HEWL caused the death of the bacteria with the destruction of the cell wall. LIVE/DEAD assays of fluorescent dye stain of the membrane cell showed membrane perturbation of bacteria after incubation with modified HEWL. The cell wall destruction was viewed using electron microscopy. The results obtained in this study suggest that heat-denatured HEWL at pH 6.0 and chemical-denatured HEWL treatments increase the HEWL antibacterial activity against Gram-negative bacteria.


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