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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
Mon Jul 01 2024
Journal Name
Russian Journal Of Organic Chemistry
Synthesis and Study of the Biological Activity of New Compounds Derived from 4-(5-Phenyl-1,3,4-oxadiazole-2-yl)aniline
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Publication Date
Tue Oct 01 2019
Journal Name
Journal Of Biotechnology Research Center
Leishmanicidal activity of Artemisinin against cutaneous Leishmaniasis, in Vitro
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Background: Cutaneous leishmaniasis (CL) is a neglected disease in tropical countries, including Iraq. Several studies have sought to examine chemotherapies for leishmaniasis treatment but most of them are of toxic and/or undesirable side effect, therefore, the need for investigating new fewer toxic therapies is essential. Aim of study: In this study, the cytotoxic effect of Artemisinin (ART), a novel herbal compound, was screened against the two forms, promastigotes and amastigotes, of the Iraqi isolate of Leishmania tropica, the causative agent of Baghdad boil. Material and methods:  Different concentrations (1000, 500, 250, 125, 62.5, 31.25, 15.6 and 7.8) µM of Artemisinin were screened to investigate the leishmanic

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Publication Date
Tue Jan 01 2019
Journal Name
Journal Of Biotechnology Research Center
Leishmanicidal activity of Artemisinin against cutaneous Leishmaniasis, in Vitro
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Background: Cutaneous leishmaniasis (CL) is a neglected disease in tropical countries, including Iraq. Several studies have sought to examine chemotherapies for leishmaniasis treatment but most of them are of toxic and/or undesirable side effect, therefore, the need for investigating new fewer toxic therapies is essential. Aim of study: In this study, the cytotoxic effect of Artemisinin (ART), a novel herbal compound, was screened against the two forms, promastigotes and amastigotes, of the Iraqi isolate of Leishmania tropica, the causative agent of Baghdad boil. Material and methods: Different concentrations (1000, 500, 250, 125, 62.5, 31.25, 15.6 and 7.8) µM of Artemisinin were screened to investigate the leishmanicidal activity of th

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Publication Date
Wed May 07 2025
Journal Name
Microbes And Infectious Diseases
Antibacterial activity of mentha piperita extraction against uropathogenic bacteria
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Publication Date
Fri Jan 01 2016
Journal Name
Kmitl Science And Technology
Antibacterial Activity of Lactobacillus buchneri Bacteriocin against Vibrio parahaemolyticus
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Eleven yoghurt samples were collected from local markets in Baghdad to isolate Lactobacillus buchneri. Only 3 isolates of L. buchneri were found and the isolate No. 3 was the most producer of bacteriocin. Bacteriocin was adsorbed 100% onto silicic acid at pH 6.0-7.0. Below or above these pH values, adsorption was decreased, ranging between 35 and 90%. Therefore, pH 6.0 was used for the purification procedure. The purification procedure including silicic acid adsorption/desorption and cation-exchange chromatography (CEC) resulted in a 11.11 fold increase in the final specific activity of pure bacteriocin (1176.47 Au/mg) compared to the culture supernatant which was 32.64 Au/mg. The molecular weight was determined to be about 3.4 kDa. The bac

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Publication Date
Wed Jan 06 2021
Journal Name
International Journal Of Pharmaceutical Research
New Polymeric Coii, Niii And Cdii Complexes With Tetrazole Schiff-Base Ligands; Synthesis, Spectral Characterisation And Biological Activity
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New Schiff-base ligands bearing tetrazole moiety and their polymeric metal complexes with Co(II), Ni(II) and Cd(II) ions are reported. Ligands were prepared in a multiple-step reaction. The reaction of sodium 2,6- diformylphenolate and cyclohexane-1,3-dione with 5-amino-2-fluorobenzonitrile resulted in the isolation of two precursors sodium 2,6-bis((E)-(3-cyano-4-fluorophenylimino)methyl)-4-methylphenolate 1 and 5,5'- (1E,1'E)-cyclohexane-1,3-diylidenebis- (azan-1-yl-1-ylidene)bis(2-fluorobenzonitrile) 2, respectively. The reaction of precursors with azide gave the required ligands; sodium 2,6-bis((E)-(4-fluoro-3-(1H-tetrazol-5- yl)phenylimino)methyl)-4-methylphenolate (NaL) and (N,N'E,N,N'E)-N,N'-(cyclohexane-1,3-diylidene)bis(4- fluoro-3-

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Publication Date
Fri Jan 01 2021
Journal Name
International Journal Of Pharmaceutical Research
New Polymeric Coii, Niii And Cdii Complexes With Tetrazole Schiff-Base Ligands; Synthesis, Spectral Characterisation And Biological Activity
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New Schiff-base ligands bearing tetrazole moiety and their polymeric metal complexes with Co(II), Ni(II) and Cd(II) ions are reported. Ligands were prepared in a multiple-step reaction. The reaction of sodium 2,6- diformylphenolate and cyclohexane-1,3-dione with 5-amino-2-fluorobenzonitrile resulted in the isolation of two precursors sodium 2,6-bis((E)-(3-cyano-4-fluorophenylimino)methyl)-4-methylphenolate 1 and 5,5'- (1E,1'E)-cyclohexane-1,3-diylidenebis- (azan-1-yl-1-ylidene)bis(2-fluorobenzonitrile) 2, respectively. The reaction of precursors with azide gave the required ligands; sodium 2,6-bis((E)-(4-fluoro-3-(1H-tetrazol-5- yl)phenylimino)methyl)-4-methylphenolate (NaL) and (N, N'E, N, N'E)-N, N'-(cyclohexane-1,3-diylidene)bis(4- fluor

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Publication Date
Wed Mar 18 2020
Journal Name
Baghdad Science Journal
Lemon juice antioxidant activity against oxidative stress
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This study is conducted to evaluate the therapeutic and antioxidant effect of lemon juice on some hematological and biochemical parameters. Thirty female mice used in this study were exposed to oxidative stress through giving them hydrogen peroxide in drinking water for 30 days. Animals randomly distributed over 3 groups, each group contained 10 animals and treated as follows: T1 control group (drinking distilled water only), T2 (0.75% hydrogen peroxide in drinking water) and T3 (0.75% hydrogen peroxide in drinking water with daily drenching with 1 mL lemon juice). At the end of the experiment, blood samples were collected from animals for evaluating the following hematological and biochemical parameters: Haemoglobin concentration (Hb),

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Publication Date
Wed Jun 28 2017
Journal Name
Iraqi Journal Of Science
Antibacterial Activity of Synergistic Effect of Colicin and Gold Nanoparticles Against Pseudomonas Aerugensa
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Publication Date
Thu Oct 01 2020
Journal Name
Systematic Reviews In Pharmacy
Estimation of activity and toxicity of silver nanoparticles loaded metronidazole against Giardia lamblia
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Giardia lamblia is one of most common protozoan cause diarrheas, and the most health problem in development countries worldwide. Our work aimed to assess activity and toxicity of metronidazole loaded silver nanoparticles in treatment of acute giardiasis in mice. After inoculated mice with Giardia cysts in a dose of 105 cyst for acute infection, treatments were given for eight days. Number Giardia cysts in stool were discovered. Toxicity nanoparticles was estimated by Measurement oxidative stress markers (GSH) and (MDA) in liver, kidney tissue homogenate. The results showed single therapy was better effect by silver nanoparticles, highest percentages of reduction in number of cysts Giardia lamblia of infected mice treated with silver nanopar

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