scholarly journals Binding of Ceftobiprole and Comparators to the Penicillin-Binding Proteins of Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Streptococcus pneumoniae

2007 ◽  
Vol 51 (7) ◽  
pp. 2621-2624 ◽  
Author(s):  
Todd A. Davies ◽  
Malcolm G. P. Page ◽  
Wenchi Shang ◽  
Ted Andrew ◽  
Malgosia Kania ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antibacterial Activity ◽  
Streptococcus Pneumoniae ◽  
Binding Proteins ◽  
Tight Binding ◽  
Gram Negative ◽  
Penicillin Binding Proteins ◽  
Gram Positive Bacteria

ABSTRACT Ceftobiprole exhibited tight binding to PBP2a in methicillin-resistant Staphylococcus aureus, PBP2x in penicillin-resistant Streptococcus pneumoniae, and PBP3 and other essential penicillin-binding proteins in methicillin-susceptible S. aureus, Escherichia coli, and Pseudomonas aeruginosa. Ceftobiprole also bound well to PBP2 in the latter organisms, contributing to the broad-spectrum antibacterial activity against gram-negative and gram-positive bacteria.

Bioactive compounds isolated from submerged fermentations of the Chilean fungus Stereum rameale

2015 ◽  
Vol 70 (3-4) ◽  
pp. 97-102 ◽  
Author(s):  
Pedro Aqueveque ◽  
Carlos Leonardo Céspedes ◽  
José Becerra ◽  
Marcelo Dávila ◽  
Olov Sterner
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antibacterial Activity ◽  
Bioactive Metabolites ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Bioassay Guided Fractionation

Abstract Liquid fermentations of the fungus Stereum rameale (N° 2511) yielded extracts with antibacterial activity. The antibacterial activity reached its peak after 216 h of stirring. Bioassay-guided fractionation methods were employed for the isolation of the bioactive metabolites. Three known compounds were identified: MS-3 (1), vibralactone (2) and vibralactone B (3). The three compounds showed antibacterial activity as a function of their concentration. Minimal bactericidal concentrations (MBC) of compound 1 against Gram-positive bacteria were as follows: Bacillus cereus (50 μg/mL), Bacillus subtilis (10 μg/mL) and Staphylococcus aureus (100 μg/mL). Compounds 2 and 3 were active only against Gram-negative bacteria. The MBC of compound 2 against Escherichia coli was 200 μg/mL. Compound 3 inhibited significantly the growth of E. coli and Pseudomonas aeruginosa, with MBC values of 50 and 100 μg/mL, respectively.

Synthesis of Chalcones and Nucleosides Incorporating [1, 3, 4]Oxadiazolenone Core and Evaluation of their Antifungal and Antibacterial Activities

2020 ◽  
Vol 15 (6) ◽  
pp. 665-679
Author(s):  
Alok K. Srivastava ◽  
Lokesh K. Pandey
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Bacillus Subtilis ◽  
Antifungal Activity ◽  
Aspergillus Niger ◽  
Gram Negative ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Good Antibacterial Activity

Background: [1, 3, 4]oxadiazolenone core containing chalcones and nucleosides were synthesized by Claisen-Schmidt condensation of a variety of benzaldehyde derivatives, obtained from oxidation of substituted 5-(3/6 substituted-4-Methylphenyl)-1, 3, 4-oxadiazole-2(3H)-one and various substituted acetophenone. The resultant chalcones were coupled with penta-O-acetylglucopyranose followed by deacetylation to get [1, 3, 4] oxadiazolenone core containing chalcones and nucleosides. Various analytical techniques viz IR, NMR, LC-MS and elemental analysis were used to confirm the structure of the synthesised compounds.The compounds were targeted against Bacillus subtilis, Staphylococcus aureus and Escherichia coli for antibacterial activity and Aspergillus flavus, Aspergillus niger and Fusarium oxysporum for antifungal activity. Methods: A mixture of Acid hydrazides (3.0 mmol) and N, Nʹ- carbonyl diimidazole (3.3 mmol) in 15 mL of dioxane was refluxed to afford substituted [1, 3, 4]-oxadiazole-2(3H)-one. The resulted [1, 3, 4]- oxadiazole-2(3H)-one (1.42 mmol) was oxidized with Chromyl chloride (1.5 mL) in 20 mL of carbon tetra chloride and condensed with acetophenones (1.42 mmol) to get chalcones 4. The equimolar ratio of obtained chalcones 4 and β -D-1,2,3,4,6- penta-O-acetylglucopyranose in presence of iodine was refluxed to get nucleosides 5. The [1, 3, 4] oxadiazolenone core containing chalcones 4 and nucleosides 5 were tested to determined minimum inhibitory concentration (MIC) value with the experimental procedure of Benson using disc-diffusion method. All compounds were tested at concentration of 5 mg/mL, 2.5 mg/mL, 1.25 mg/mL, 0.62 mg/mL, 0.31 mg/mL and 0.15 mg/mL for antifungal activity against three strains of pathogenic fungi Aspergillus flavus (A. flavus), Aspergillus niger (A. niger) and Fusarium oxysporum (F. oxysporum) and for antibacterial activity against Gram-negative bacterium: Escherichia coli (E. coli), and two Gram-positive bacteria: Staphylococcus aureus (S. aureus) and Bacillus subtilis(B. subtilis). Result: The chalcones 4 and nucleosides 5 were screened for antibacterial activity against E. coli, S. aureus and B. subtilis whereas antifungal activity against A. flavus, A. niger and F. oxysporum. Compounds 4a-t showed good antibacterial activity whereas compounds 5a-t containing glucose moiety showed better activity against fungi. The glucose moiety of compounds 5 helps to enter into the cell wall of fungi and control the cell growth. Conclusion: Chalcones 4 and nucleosides 5 incorporating [1, 3, 4] oxadiazolenone core were synthesized and characterized by various spectral techniques and elemental analysis. These compounds were evaluated for their antifungal activity against three fungi; viz. A. flavus, A. niger and F. oxysporum. In addition to this, synthesized compounds were evaluated for their antibacterial activity against gram negative bacteria E. Coli and gram positive bacteria S. aureus, B. subtilis. Compounds 4a-t showed good antibacterial activity whereas 5a-t showed better activity against fungi.

Chemical Constituents and Antibacterial Activity of Euphorbia altotibetica

2014 ◽  
Vol 881-883 ◽  
pp. 21-24
Author(s):  
Ai Mei Yang ◽  
Xiao Long Shi ◽  
Jie Li Liu ◽  
Lin Yang ◽  
Yun Men
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antibacterial Activity ◽  
Streptococcus Pneumoniae ◽  
Bacillus Licheniformis ◽  
Chemical Constituents ◽  
Etoac Extract

Five compounds were isolated from the EtOAc extract of Euphorbia altotibetica. The structures of these compounds were elucidated as: β-sitosterol (1), daucosterol (2), chrysophanol (3), (-)-epiafzelechin (4), 5,2-dihydroxy-7,8,6-trimethoxyflavanone (5) by NMR datas, the antibacterial activity of all compounds were examined on five species of bacteria Escherichia coli, Staphylococcus aureus, Bacillus licheniformis, Pseudomonas aeruginosa and Streptococcus pneumoniae.

scholarly journals Affinity of Tomopenem (CS-023) for Penicillin-Binding Proteins in Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa

2008 ◽  
Vol 53 (3) ◽  
pp. 1238-1241 ◽  
Author(s):  
Tetsufumi Koga ◽  
Chika Sugihara ◽  
Masayo Kakuta ◽  
Nobuhisa Masuda ◽  
Eiko Namba ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Binding Proteins ◽  
Binding Protein ◽  
Penicillin Binding Protein ◽  
Penicillin Binding Proteins ◽  
E Coli ◽  
High Affinity

ABSTRACT Tomopenem (formerly CS-023), a novel 1β-methylcarbapenem, exhibited high affinity for penicillin-binding protein (PBP) 2 in Staphylococcus aureus, PBP 2 in Escherichia coli, and PBPs 2 and 3 in Pseudomonas aeruginosa, which are considered major lethal targets. Morphologically, tomopenem induced spherical forms in E. coli and short filamentation with bulges in P. aeruginosa, which correlated with the drug's PBP profiles. The potential of resistance of these bacteria to tomopenem was comparable to that to imipenem.

scholarly journals Screening of some plant materials used in South-West Algerian traditional medicine for their antibacterial activity

2017 ◽  
Vol 9 (4) ◽  
pp. 619
Author(s):  
Fatehi Naima ◽  
Houcine BENMEHDI ◽  
Allali Hocine ◽  
Oulednecir Nawal
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antibacterial Activity ◽  
Traditional Medicine ◽  
Diffusion Method ◽  
Plant Materials ◽  
Gram Negative ◽  
Maximum Inhibition ◽  
Reference Strains

<p>The initial introduction of new medicinal agents into the health care system sometimes, requires information beyond that is recorded in libraries relying instead, on reports available through traditions and healers within a society. This paper explored the antibacterial activity of aqueous and hydromethanolic extracts of nine folkloric medicinal plant from Bechar region (southwest Algeria) namely: <em>A. nardus, A. schoenanthus, G. vulgaris, </em>two species of<em> H. scoparia green &amp; red, P. laevigata, R. tripartita, T. gallica</em> and <em>T. nudatum</em>, frequently used in the local traditional medicine. The antibacterial activity of different extracts were evaluated by using disc diffusion method agar and antibiotics susceptibility of ten selected microorganisms: seven reference strains, <em>Bacillus cereus, Enterococcus faecalis, Staphylococcus aureus</em>,<em> Escherichia coli</em>,<em> Klebsiella pneumoniae, Pseudomonas aeruginosa</em>, <em>Salmonella typhi</em>, and three clinically isolated strains, <em>Escherichia coli</em> (Urinary Tract Infection), <em>Escherichia coli</em> (Vaginal Infection) and <em>Staphylococcus aureus </em>(Skin Infection).</p><p>The maximum antibacterial activity was recorded against the gram negative reference strains <em>Pseudomonas aeruginosa</em>and<em> Escherichia coli</em> with a maximum inhibition diameter of 15.6 ± 0.5 and 15.0 ± 1.4 mm respectively displayed by the aqueous extract of <em>T. gallica, </em>followed by the activity detected by the hydromethanolic extract of <em>R. tripartita</em> against the gram negative reference strain <em>Pseudomonas aeruginosa </em>(14.6±1.2 mm) and the aqueous and hydromethanolic extracts of <em>R. tripartita</em> against the gram negative reference strains <em>Pseudomonas aeruginosa</em> and<em> Escherichia coli</em> with a maximum inhibition diameter of 14.3 ± 2.0 and 14.3±0.5 mm, respectively.</p><p>According to the present study, <em>H. scoparia red, P. laevigata, R. tripartita, and T. gallica</em>can be served as broad spectrum antibiotic and used as a potent source of natural antibacterial agents by replacing commercially available synthetic drug that may have a large number of side effects.</p>

scholarly journals Sintesis dan Uji Aktivitas Antibakteri Senyawa N-fenil-4-klorobenzamida

2018 ◽  
Vol 6 (2) ◽  
pp. 212
Author(s):  
Elok Dea Orens Ubung Wisnu ◽  
Indah Purnama Sary ◽  
Dwi Koko Pratoko
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antibacterial Activity ◽  
Antibacterial Agent ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Crystal Shape ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Benzamide Derivatives

N-phenylbenzamide is benzamide derivatives, which is potential as an antibacterial agent. N-phenyl-4-chlorobenzamide is N-phenylbenzamide derivative that substitued by chloro to the para position and it was expected to enhance the antibacterial activity. N-phenyl-4-chlorobenzamide was synthesized by reacting 1,3-diphenyilthiourea and 4-chlorobenzoil chloride. This compound has been purified and provided 53% of product with crystal shape, white color, and melting point of 195-197 oC. The purification of this compound was confirmed by TLC and the structure was identified by 1H-NMR, 13C-NMR, and FTIR spectroscopy. This compound was tested for its activity against gram positive bacteria Staphylococcus aureus and gram negative bacteria Pseudomonas aeruginosa, evaluated by well diffusion method and the result showed no activity against both Staphylococcus aureus and Pseudomonas aeruginosa.   Keywords: N-phenyl-4-chlorobenzamide, synthesis, antibacterial activity

Green Synthesis of Novel ethyl 3-amino-5-(methylthio)-4-(5-substituted phenyloxazol-2-yl)thiophene-2-carboxylate derivatives

2021 ◽  
pp. 105-110
Author(s):  
Satish M. Chavan
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Candida Albicans ◽  
Aspergillus Niger ◽  
Microwave Irradiation ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
Green Protocol ◽  
Gram Positive Bacteria

Synthesis of novel ethyl 3-amino-5-(methylthio)-4-(5-substituted phenyloxazol-2-yl) thiophene-2-carboxylate derivatives from 3-amino-4-carbamoyl-5-(methylthio)thiophene-2-carboxylate was carried out by traditional as well as microwave irradiation green protocol. Ethyl 3-amino-5-(methylthio)-4-(5-substituted phenyloxazol-2-yl) thiophene-2-carboxylate derivatives were screened for antimicrobial screening against gram positive bacteria Staphylococcus aureus (ATCC 29737), gram negative bacteria Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853) and Candida albicans (MTCC 277), Aspergillus niger (MCIM 545) fungi.

scholarly journals Reactions of tin- and triorganotin(IV) isopropoxides with thymol derivative: Synthesis, characterization and in vitro antimicrobial screening

2013 ◽  
Vol 78 (9) ◽  
pp. 1323-1333 ◽  
Author(s):  
Garima Matela ◽  
Robina Aman ◽  
Chetan Sharma ◽  
Smita Chaudhary
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Nuclear Magnetic Resonance ◽  
Antibacterial Activity ◽  
Gram Negative Bacteria ◽  
Carboxylate Group ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
1H Nuclear Magnetic Resonance

A new series of diisopropyloxytin- and triorganotin(IV) complexes of H2hbgl (1) of the general formula Sn(OPri)2(hbgl) (2), Sn(OPri)2(Hhbgl)2 (3), Ph3Sn(Hhbgl) (4), Bu3Sn(Hhbgl) (5) and Me3Sn(Hhbgl) (6), [where H2hbgl= a ligand of thymol derivative namely, N-(2-hydroxy-3-isopropyl-6-methyl benzyl)Glycine] were synthesized by reacting tin- and triorganotin(IV) chloride with the ligand, with the aid of sodium iso-propoxide in appropriate stiochiometric ratios (1:1 and 1:2). These complexes were characterized by elemental analysis, IR, 1H nuclear magnetic resonance. The spectral data suggest that the carboxylate group, in complexes 2-5, was bonded in a bidentate manner, while a unidentate bonding was observed in complex 6. All five complexes were tested in vitro for their antibacterial activity against Gram-positive bacteria namely, Staphylococcus aureus MTCC 96, Bacillus subtilis MTCC 121 and two Gram-negative bacteria namely, Escherichia coli MTCC 1652 and Pseudomonas aeruginosa MTCC 741. All the five complexes were also tested against three pathogenic fungal strains namely, Aspergillus niger, A. flavus and Penicillium sp.

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