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Synthesis of New Cephalosporins of Expected Improved Activity and Resistance Against -Lactamases
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The development of new cephalosporins with improved activity against resistant microbes, such as, MRSA (methicillin resistant Staph. aureus), P. aeruginosa, is of high potential. Chemical synthesis of two new series of thiadiazole linked to cysteine (series 1) and cephalosporins containing thiadiazole linked to cysteine through disulfide bond (series 2) were achieved. The chemical structures of the synthesized compounds were confirmed using spectral (FT-IR, 1H-NMR) and elemental microanalysis. The incorporation of privileged chemical moieties, such as, thiadiazole, Schiff base, cysteine and sulfonamide, has been found to have great contribution to the antimicrobial activities. Compounds of series 1 (1b-d), containing a Schiff base or a sulfonamido moiety, showed reasonable activity and were less potent than cephalexin with respect to E. coli and Staph. aureus. The new cephalosporins (series 2) showed remarkable activities on E. coli (62.5-15.6µg/ml) and staph. aureus (31.2-62.5µg/ml) when compared with cephalexin (250 and 125 µg/ml) respectively. Moreover, compounds 1 and 3 showed very promising activity against MRSA (250 and 500µg/ml) respectively. The incorporation of a sulfonamido moiety to the cephalosporin molecule was successfully achieved. This is a very interesting finding which may open a new approach in the synthesis of newer cephalosporins.   

Keywords: Cephalosporins, Cysteine, Schiff base, Sulfonamides, Thiadiazole.

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Publication Date
Wed Jun 01 2022
Journal Name
Baghdad Science Journal
Syntheses, Structures and Biological Activity of Some Schiff Base Metal Complexes
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Four new binuclear Schiff base metal complexes [(MCl2)2L] {M = Fe 1, Co 2, Cu 3, Sn 4, L = N,N’-1,4-Phenylenebis (methanylylidene) bis (ethane-1,2-diamine)} have been synthesized using direct reaction between proligand (L) and the corresponding metal chloride (FeCl2, CoCl2, CuCl2 and SnCl2). The structures of the complexes have been conclusively determined by a set of spectroscopic techniques (FT-IR, 1H-NMR, and mass spectra). Finally, the biological properties of the complexes have been investigated with a comparative approach against different species of bacteria (E. coli G-, Pseudomonas G-, Bacillus G+,

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Publication Date
Mon Jan 01 2024
Journal Name
Medical Journal Of Babylon
Characterization and antibacterial activity of biogenic iron nanoparticles using Proteus mirabilis
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Abstract<sec> <title>Background:

The green production of iron oxide nanoparticles (FeONPs) due to its numerous biotechnological uses has attracted a lot of attention and clean and eco-friendly approaches in the medical field.

Objectives:

The objectives of this study are to demonstrate the biogenic creation of FeONPs. The search for alternative antimicrobial medicines has been prompted by growing worries about multidrug resistance.

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Publication Date
Thu Apr 20 2023
Journal Name
Baghdad Science Journal
Ni2+, Pt4+, Pd2+, and Mn2+ Metal ions Complexes with Azo Derived from Quinolin-2-ol and 3-amino-N-(5-methylisoxazol-3-yl) Benzenesulfonamide: Synthesis, Characterization, Thermal Study ,and Antioxidant Activity
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  Diazotization reaction between quinolin-2-ol and (2-chloro-1-(4-(N-(5-methylisoxazol-3-yl)sulfamoyl)phenyl)-2l4-diazyn-1-ium was carried out resulting in ligand-HL, this in turn reacted with the next metal ions (Ni2+, Pt4+, Pd2+, and Mn2+)  forming stable complexes with unique geometries such as (tetrahedral for both Ni2+ and Mn2+, octahedral for Pt4+ and square planer for Pd2+ ). The creation of such complexes was detected by employing spectroscopic means involving ultraviolet-visible which proved the obtained geometries, fourier transfer proved the formation of azo group and the coordination with metal ion through it. Pyrolysis (TGA & DSC) studies proved the coordination of water residues with metal ions inside the coordin

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Publication Date
Fri Dec 01 2023
Journal Name
Baghdad Science Journal
Ni2+, Pt4+, Pd2+, and Mn2+ Metal ions Complexes with Azo Derived from Quinolin-2-ol and 3-amino-N-(5-methylisoxazol-3-yl) Benzenesulfonamide: Synthesis, Characterization, Thermal Study ,and Antioxidant Activity
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Diazotization reaction between quinolin-2-ol and (2-chloro-1-(4-(N-(5-methylisoxazol-3-yl)sulfamoyl)phenyl)-2l4-diazyn-1-ium was carried out resulting in ligand-HL, this in turn reacted with the next metal ions (Ni2+, Pt4+, Pd2+, and Mn2+)  forming stable complexes with unique geometries such as (tetrahedral for both Ni2+ and Mn2+, octahedral for Pt4+ and square planer for Pd2+ ). The creation of such complexes was detected by employing spectroscopic means involving ultraviolet-visible which proved the obtained geometries, fourier transfer proved the formation of azo group and the coordination with metal ion through it. Pyrolysis (TGA &

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Publication Date
Fri Jan 01 2016
Journal Name
Chemistry And Materials Research
Synthesis of Triazolo and Pyrazolo Derivatives of Quinoline Nucleus
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New heterocyclic derivatives of quinoline are reported. Reaction of quinoline-2-thiol 4 with hydrazine hydrate gave 2-hydrazionoquinoline 5. Treatment of 5 with CS2 in pyridine afforded 1,2,4-triazolo-[4,3-a]- quinolin-1-2H-thione 6, whereas the reaction of 5 with carboxylic acids namely formic acid or acetic acid, yielded the 1,2,4-triazol-[4,3-a]-quinolin 7 or 5-methyl-1,2,4-triazolo [4,3-a]-quinoline 8 through ring closure. Diazotization of 5 under acidic conditions produced the fused tetrazole compound 9, tetrzolo-[1,5-a]- quinoline. Moreover, treatment of 5 with active methlyene compounds gave two pyrazole derivatives 10 and 11. Azomethines 12a-e were prepared through condensation of 5 with aromatic aldehydes or ketones.

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Publication Date
Sun Dec 25 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Atimicrobial Evaluation of Deuterated Analogues of Metronidazole
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The discovery of novel therapeutic molecules is always difficult, and there are a variety of methodologies that use the most diverse and innovative medicinal chemistry approaches. One such approach is the deuteration technique: Deuteration is the process of substituting deuterium for hydrogen in a molecule. When compared to the drug molecule, its deuterated analogues may retain the features of the original molecule and, in some cases, improve its pharmacological activity, with fewer side effects and lower toxicity. Metronidazole is a commonly used antibiotic to treat anaerobic bacterial infections, protozoal and microaerophilic bacterial infections. Met

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Publication Date
Thu Apr 20 2017
Journal Name
International Journal Of Science And Research (ijsr)
Effect of Different Sealer Systems on the Resistance to Vertical-Root-Fracture of Endodontically Treated Tooth
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Abstract: An unfavorable complication of root canal is vertical root fracture. The aim of present study is to evaluate the vertical root fracture of treated teeth filled with gutta percha and Resilon obturating material using different sealers. Forty mandibular premolars used in the study. Canals randomly divided into four groups (n=10). Group-A eugenol-based (Endofill) sealer with gutta percha; GroupB epoxy-amine (AH Plus) sealer with gutta percha; Group-C resin-based (Real Seal) sealer with Resilon; or Group-D epoxide-based (Perma Evolution) sealer with gutta percha. Roots mounted vertically in cold cure acrylic blocks and subjected to vertical loading with a crosshead speed of 1mm ̸min. The point at which fracture of the roots occurred

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Publication Date
Sat Jan 01 2022
Journal Name
Journal Of The Mechanical Behavior Of Materials
The effect of using different fibres on the impact-resistance of slurry infiltrated fibrous concrete (SIFCON)
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Abstract<p>Slurry infiltrated fibrous concrete (SIFCON) is a modern type of fibre reinforced concrete (FRC). It has unique properties; SIFCON is superior in compressive strength, flexural strength, tensile strength, impact resistance, energy absorption and ductility. Because of this superiority in these characteristics, SIFCON was qualified for applications of special structures, which require resisting sudden dynamic loads such as explosions and earthquakes. The main aim of this investigation is to determine the effect of fibre type on the apparent density of SIFCON and on performance under impact load. In this investigation, hook-end steel fibre and polyolefin fibre were used. Purely once and </p> ... Show More
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Publication Date
Fri Jan 27 2023
Journal Name
Research Journal Of Pharmacy And Technology
Physical human Activity, Immunity and COVID-19
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Background: The global threat of COVID-19 outbreak and on the 11 March 2020, WHO acknowledged that the virus would likely spread to all countries across the globe and declared the coronavirus outbreak a pandemic which is the fifth pandemic since 20 century and this has brought human lives to a sudden and complete lockdown and the confirmed cases of this disease and deaths continue to rise in spite of people around the world are taking important actions to mitigate and decrease transmission and save lives. Objectives: To assess the effect of exercise and physical activity on the immunity against COVID-19. Methods: Collected electronic databases including (Medline, EMBASE, Google Scholar, PubMed and Web of Science) were searched with

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Publication Date
Wed Jun 01 2022
Journal Name
International Journal Of Nanoscience
Zinc Oxide Nanoparticle Properties and Antimicrobial Activity
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In this study, zinc oxide was prepared by pulsed laser ablation method (PLAL), which is an easy-to-use and inexpensive physical method. The optical properties were studied using UV-Vis spectrometers, structure properties by (XRD) to calculate the crystalline size, and particle size determination by Field emission scanning electron microscopy (FE-SEM) and (EDS), transmission electron microscopy (TEM) assays and it was proved that they are within the ideal nanoscale for biological application. These ZnO NPs were employed on the inhibitory activity of different types of Gram-positive and Gram-negative bacteria, as well as on fungi, and it was noted their ability to penetrate the bacterial cell wall and inhibit its action.

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