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Synthesis of new derivatives of Ceftazidime as possible Prodrugs
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Five new ceftazidime derivatives were designed and synthesized in an attempt to improve the acid stability and may increase the spectrum of ceftazidime. The synthesized compounds included;  Schiff base of ceftazidime (compound 1), ceftazidime lysine amide Schiff base (compound 2), ceftazidime lysine amide (compound 3), ceftazidime-di-lysine amide Schiff base (compound 4) and ceftazidime-di-lysine amide (compound 5). New ceftazidime derivatives were successfully prepared characterized and identified using spectral and elemental microanalysis (CHNS) analyses and the results comply with the calculated measurements.

Compounds 1 and 2 were subjected to a stability study in phosphate buffer (0.2M, pH 7.4) and in KCl/HCl buffer (0.2M, pH 1.2) at different time intervals (0 – 240 min) incubated at 37 °C. This revealed that both compounds in phosphate buffer (0.2M, pH 7.4) are significantly stable with t 1/2 of 18hrs and 24hrs respectively. However, compounds 1 and 2 are less stable in KCl/HCl buffer (0.2M, pH 1.2) with t1/2 of 3.48hrs and 3.13hrs respectively.

The antibacterial evaluation of the new ceftazidime derivatives showed various degrees of antibacterial activities when compared with ceftazidime. The chemical modifications of ceftazidime showed slight effect on activities and most of compounds retained the antibacterial activities. Compounds 2 and 4  afforded comparable antibacterial action. However, compounds 3 and 5 were equipotent with ceftazidime with respect to E.coli and Staph. aureose. Compound 4 has better activity than ceftazidime with respect to Pseudomonas  aeruginosa. Schiff's base derivative of lysine (2, 6-bis-(benzylideneamino) hexanoic acid) gave a reasonable antibacterial action towards Escherichia coli and Streptococcus Spp; as compared with lysine which has no antibacterial activity.

Key words: Ceftazidime, Schiff bases, Lysine.

 

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Publication Date
Sat Dec 24 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Possible protective effects of two different doses of cyanocobalamin against methotrexate nephrotoxicity in rats
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Abstract

   Nephrotoxicity is defined as rapid deterioration in kidney functions. It arises from direct exposure to drugs or their metabolites. Methotrexate is a famous chemotherapeutic drug with anti-inflammatory and immunosuppressive properties. A high-dose methotrexate-induced renal dysfunction can be life threatening. Cyanocobalamin, one of the forms of vitamin B12, acts as a coenzyme in the conversion of homocysteine to methionine in the cytosol, and the conversion of methylmalonyl-CoA to succinyl-CoA in the mitochondrion. This study is designed to examine the effect of cyanocobalamin in two different doses each co-administered with methotrexate at 20 mg/kg induced nephrotoxicity in rat

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Publication Date
Fri Nov 03 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Possible Protective Effect of Low Dose of Papaverine on ANIT Induce Cholestasis in Rat
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Abstract Intrahepatic cholestasis is clinical syndrome which cause either by defect in synthesis or bile acid flow, the pathophysiology of cholestasis is complicated by a number of  variables, including oxidative stress, inflammatory response, and  dysregulation of bile acid transporter . Rats, mice, and guinea pigs were utilized as experimental animals, and ANIT was administered to them in order to create a model that closely resembled intrahepatic cholestasis in human. This study examined the protective effects of papaverine, a non-narcotic opium alkaloid derived from papaver somniferum and discovered as an FXR agonist, on cholestasis in rats induced by alpha-naphthylisothiocyanate (ANIT). Rats utilized in this study divid

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Publication Date
Sun Nov 01 2020
Journal Name
Journal Of Physics: Conference Series
Synthesis, Characterization, Antibacterial study and Efficiency of Inhibition of New di-β-enaminone Ligand and its Complexes
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Abstract<p>The new ligand [3,3’-(1,2-phenylenebis(azanediyl))bis(5,5-dimethylcyclohex-2-en-1-one)] (L) derived from 5,5-Dimethylcyclohexane-1,3-dione with 1,2-phenylenediamine was used to prepare a new chain of metal complexes of Mn(ii), Co(ii), Ni(ii), Cu(ii), Cd(ii) and Zn(ii) by inclusive formula [M(L)]Cl2. Characterized compounds on the basis of <sup>1</sup>H, <sup>13</sup>CNMR (for ligand (L)), FT-IR and U.V spectrum, melting point, molar conduct, %C, %H and %N, the percentage of the metal in complexes %M, Magnetic susceptibility, thermal studies (TGA), while its corrosion inhibition for (plain steel) in tap water is studied by weight loss. These measurements proved th</p> ... Show More
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Publication Date
Sun Sep 05 2010
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New Metal Complexes of &#945;-Aminonitriles Derived from P- Toluidine and Aromatic Aldehydes
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New metal complexes of some transition metal ions Co(II), Cu(II) , Cd(II) and Zn(II) were prepared by their reaction with previously prepared ligands HLI= (P-methyl anilino) phenyl acetonitrile and HLII = (P-methyl anilino) –P– chloro phenyl acetonitrile . The two ligands were prepared by Strecker’s procedure which includ the reaction of p- toluidine with benzaldehyde and P- chlorobenzaldehyde respectively. Structures were proposed depending on atomic absorption , i.r. and u.v.visible spectra in addition to magnetic susceptibility and electrical conductivity measurements.

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Publication Date
Tue Jan 01 2013
Journal Name
Ibn Al-haitham Jour. For Pure & Appl. Sci.
Synthesis And Characterization Of Some New Metal Complexes Of Ethyl Cyano (2-Methyl Carboxylate Phenyl Azo Acetate)
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Complexes of (Co2+, Ni2+, Cu2+, Zn2+, Cd2+ and Hg2+) with the ligand Ethyl cyano (2-methyl carboxylate phenyl azo acetate) (ECA) have been prepared and characterized by FTIR, (UV-Visible), Atomic absorption spectroscopy, Molar conductivity measurements and magnetic moments measurements. The following general formula has been suggested for the prepared complexes [M(ECA)2]Cl2 where M = (Co2+, Ni2+, Cu2+ ,Zn2+, Cd2+, Hg2+) and the geometry is octahedral.

Publication Date
Wed Feb 28 2018
Journal Name
International Journal Of Science And Research (ijsr)
Synthesis, Structure Determination and Biological Study of Some Complexes of New Ligand Derived from L-ascorbic Acid
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2,2'-(1-(3,4-bis(carboxydichloromethoxy)-5-oxo-2,5-dihydrofuran-2-yl)ethane-1,2-diyl)bis(oxy)bis(2,2-dichloroacetic acid) a derivative of L-ascorbic acid was prepared by reaction of L-ascorbic acid with trichloroacetic acid (1:4) ratio, in the presence of potassium hydroxide. A series of new metal complexes of this ligand were prepared by a reaction with the chlorides of Cd(II), Co(II), Ni(II), Cu(II) and Zn(II). The new ligand and its complexes were identified by C.H.N., IR, UV-visible spectra, Thermogravimetric analysis (TGA), as well as 1H, 13C-NMR and Mass spectra for ligand L. The complexes were also identified by molar conductance, atomic absorption, magnetic susceptibility and X-ray diffraction for Cu (II) complex. FT-IR spectra

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Publication Date
Thu Dec 01 2022
Journal Name
Russian Journal Of Bioorganic Chemistry
Synthesis, Identification and Study of Antioxidant and Anticancer Activities of New 2-Substituted-1,3,4-Thiadiazole from Creatinine
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Publication Date
Sat Jan 16 2016
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis, Characterization And Biological Evaluation of New Schiff Bases Mixed Ligand Metal Complexes of Some Drug Substances
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Publication Date
Fri Aug 17 2001
Journal Name
Molecular Crystals And Liquid Crysta
Synthesis, characterization and study of mesomorphic behavior of new bent and linear core compounds containing heterocyclic rings
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The article presents the synthesis and liquid crystalline properties of some of new bent and linear core compounds containing a 1,3,4-oxadiazole, piperazine and thiazolidin-4-one rings as a central core. The new synthesized compounds were characterized by elemental analysis and FTIR, ¹HNMR and mass spectroscopy). The liquid crystalline properties were studied by polarized optical microscopy and differential scanning calorimetry. All Schiff bases compounds with 1,3,4-oxadiazole and piprzaine ring in central core presented liquid crystalline properties. The liquid crystallinity of compounds containing 1,3,4-oxadiazole and thiazolidin-4-one rings as a central core were found depending on the type of terminal substituents.

Publication Date
Mon Dec 20 2021
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New nano catalyst Mo-Ni /TiO2- γAl2O3 for Hydrodesulphurization of Iraqi Gas Oil
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   A new nano-sized NiMo/TiO2-γ-Al2O3 was prepared as a Hydrodesulphurization catalyst for Iraqi gas oil with sulfur content of 8980 ppm, supplied from Al-Dura Refinery. Sol-gel method was used to prepare TiO2- γ-Al2O3 nano catalyst support with 64% TiO2, 32% Al2O3, Ni-Mo/TiO-γ-Al2O3 catalyst was prepared under vacuum impregnation conditions to loading metals with percentage 3.8 wt.% and 14 wt.% for nickel and molybdenum respectively while the percentage for alumina, and titanium became 21.7, and 58.61 respectively. The synthesized TiO2- γ-Al2O3 nanocomposites and Ni-Mo /TiO2

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