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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
Tue Apr 30 2024
Journal Name
International Journal Of Phytopathology
Role of Arbuscular Mycorrhiza (AM) Fungi and Lignin in Biological Control against Vascular Fusarium Wilt Disease
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The current study aimed to assess the biological efficacy of the triple arbuscular mycorrhiza (AM) mixture of fungi Glomus etunicatum, G. leptotichum and Rhizophagus intraradices, and mix it with organic matter (O) and pathogenic fungi Fusarium oxysporum f.sp.lycopersici by using voyeurism in the plastic house in the growth of the tomato plant after four and eight weeks of cultivation. The results were shown after the treatment of the tomato plant in agriculture with the mixture of mycorrhiza and the pathogenic fungi and organic matter were treated with the mixture of mycorrhiza, organic matter and pathogenic fungi together. The effect of mycorrhiza and organic matter interference on the increase in the percentage of the lignin afte

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Publication Date
Sun Nov 01 2020
Journal Name
Iop Conference Series: Materials Science And Engineering
Protective effect of red cabbage and garlic extracts against Fumonisin B1 induced hepatotoxicity in male mice
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Abstract<p>Red cabbage and garlic extracts have protective effect against liver damage induced by fumonisin B1 (FB1) in male mice was studied. Randomly sixty mice have been divided in to six groups. Group one are the healthy mice, Group two are mice received oral dose of only FB-1 (100 μg/kg.b.w) once on daily for 1 month, Group three: mice received with red cabbage extract (500 mg/kg.bw) plus FB1, Group four: mice receiving just red cabbage extracts, Group five: mice receiving garlic extract (500mg/kg.bw) plus FB1, group 6: mice received only garlic extract. After finished the experiment, samples of blood were used for biochemical examination. The results indicated that group (2) mice treated </p> ... Show More
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Publication Date
Thu Jan 01 2015
Journal Name
Journal Of Madenat Alelem College
Antimicrobial effect of Trigonella foenum graecum Seed Extracts against Tested Bacteria Isolated from Meat and Fish
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A qualitative chemical test was performed on functional groups extracted from fenugreek plant and its extracts (aqueous, alcoholic and volatile oil). Results revealed that fenugreek seeds contain the main functional groups, while extracts are varied accorodihg to their content of functional groups qualitatively and quantitively. Moreover, inhibition activity was tested for extracts of fenugreek seeds (aqueous, alcoholic and volatile oil). against gram negative (Salmonella typhimurium, Escherichia coli and Pseudomonas aeruginosa) and gram positive (Staphylococcus aureus) by the ager well diffusion method. Data have revealed that inhibition activity was different in accoradance with extract solvent and the tested microorgan. Oil extract (15)%

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Publication Date
Sat Dec 11 2021
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Evaluation of Synergistic Antibacterial Effect of Combined Scrophularia striata Extract and Antibiotics Against Pseudomonas aeruginosa and Methicillin -Resistant Staphylococcus aureus
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Scrophularia. striata from Scrophulariacea family has been used in Iranian folk medicine for the treatment of infectious diseases. In this study we evaluated the synergistic effect of S. striata   hydroalcoholic extract (SSE) and commercially available antibiotics against P. aeroginosa and Methicillin- resistant Staphylococcus aureus (MRSA). The resazurin-based microdilution method was used to determine the minimum inhibitory concentration (MIC) values of plan extract and standard antibiotics. The interaction between standard antibiotics and SSE was evaluated by using checkerboard method. The results of this study revealed that SSE enhance the antibacterial activity of antibiotics. The combin

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Publication Date
Tue May 01 2018
Journal Name
Journal Of Physics: Conference Series
The study of Bacteriocin of Pseudomonas fluorescens and Citrus limon effects against Propionibacterium acnes and Staphylococcus epidermidis in acne patients
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Research was carried out antibacterial of (Citrus limon) juice on Acnevulgaris. Samples were obtained from individuals having (Pimples) by swabbing their faces. Substances natural from plants are promising to treat disease cause Acnevulgaris, the study in vitro biological activity of the juice, as well as bacterocin cultivated and fruits was investigated on two strain bacteria (Propionibacterium acnes, Staphylococcus epidermidis). The new antimicrobial (bacteriocin and Citrus juice) is ongoing search. This study used s juice at different concentrations at (20%, 30%, 40%, 60%, 80% and 100%). The Bacteriocin produced from local P. fluorescens isolates from wound infection and majority of isolates were found to produce crude Bacteriocin were (

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Publication Date
Sun May 28 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
The Effect of Lactobacillus gasseri Against Pseudomonas aeruginosa Infection in Mice.
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    The effect of local Lactobacillus gasseri filtrate against Pseudomonas aeruginosa infection in mice was studied . 0.25 ml of concentrated filtrate Lactobacillus gasseri was injected in intraperitoneally ( I.P.) 5 days before challenge with 0.2 ml  viable  P. aeruginosa ( 10 8  cell/ ml).       Animals were sacrificed after 12 h. from challenge by cutting the femoral artery . To follow bacterial growth in the peritoneal cavity , its contents were washed out with 5 ml of  PBS .The fluid was diluted, 0.1 ml from each dilution and was spread on culture media. The number of colonies in 5 ml of harvested fluid was expressed as Log 10 CFU ,and the percentage of Macrophage in t

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
The Protective Effect of Honey Against Amikacin- induced Nephrotoxicity in Rats
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Drug –induced nephrotoxicity is an important cause of renal failure. Aminoglycoside antibiotics, such as amikacin, which causes ototoxicity and nephrtotoxicity as a main side effects, this is focused on the use of natural materials as antioxidants against the toxic oxidative action that exert a cell damaging effect. The most important one of these materials is the honey. The aim of this work is to evaluate the antioxidant effects of honey against amikacin – induced nephrotoxicity.18 albino rats divided into 3 groups (6 rats per each group), group 1 received I.P daily dose of normal saline (control), group 2 received (35  mg/kg/day) I.P dose of amikacin ,and group 3 received (35mg/kg/day) of amikacin I.P dose in combina

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Publication Date
Sun Jun 12 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
The Ameliorative Effect of Fimasartan against Methotrexate-Induced Nephrotoxicity in Rats
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Drug-induced acute kidney injury is a serious disorder. Oxidative stress has a key role in its initiation and progression. In this study, the possible ameliorative effect of fimasartan against methotrexate-induced nephrotoxicity was investigated in comparison with α-tocopherol in rats. Wistar rats were allocated into six groups and treated as follows: group Ӏ received water on a daily basis for 8 successive days; group ӀӀ received methotrexate (20 mg/kg) on day 1, followed by water for 7 successive days; group ӀӀӀ received fimasartan (3 mg/kg/day) for 7 successive days; group IV received α-tocopherol (1 g/kg/day) for 7 successive days; group V re

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Publication Date
Mon Sep 30 2013
Journal Name
Iraqi Journal Of Science
Protective Effect of Vitamin A against Oxidative Stress Caused by Methotrexate
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Methotrexate (MTX), a folate antagonist agent, is mainly used in treatment of malignant tumors and autoimmune diseases. The present study was undertaken to determine whether antioxidant vitamin (vitamin A) could ameliorate methotrexate induced oxidative stress in male rabbits. Twenty male rabbits were randomly assigned into four groups. Group 1: control group, Group 2: MTX-treated group (received 20 mg/kg MTX intraperitoneally), Group 3: Vit.A treated group received 5000 IU Vit.A orally) and Group 4: MTX+Vit.A treated group received MTX 20 mg/kg plus 5000 IU vit.A). After 4 weeks of treatment, blood samples were collected by cardiac puncture to determine the serum malondialdehyde (MDA), as a good indicator for lipid peroxidation and

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Publication Date
Sat Jan 01 2011
Journal Name
North American Journal Of Medical Sciences
Antagonistic effect of bacteriocin against urinary catheter associated Pseudomonas aeruginosa biofilm
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