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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
Tue Jun 20 2023
Journal Name
Baghdad Science Journal
Preparation, characterization, antioxidant activity of 1-(2-furoyl) thiourea derivatives and study the molecular docking of them as potent inhibitors of Urease enzyme
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In this work, we synthesized thirteen compounds of 1-(2-furoyl)thiourea derivatives 1-13 by conversion of 2-furoyl chloride to 2-furoyl isothiocyanate by reacting it with potassium thiocyanate in dry acetone in a quite short reflux time then, in the same pot, different of (primary and secondary amines) were added individually to achieve thiourea derivatives. The products were characterized spectroscopically using (FT-IR, 1H NMR and 13C NMR) techniques. Some of them were evaluated as antioxidant agents using DPPH radical scavenging method, and all were examined theoretically as enzyme inhibitors against Bacillus pasteurii urease (pdb id: 4ubp) and  by studying  molecular docking using Autodock (4.2.6) software.

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Publication Date
Tue Feb 01 2022
Journal Name
Macromolecular Symposia
Synthesis of 5‐Fluorouracil–Naproxen Conjugates as a Mutual Prodrug for Targeting Cancer Tissues
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Abstract<p>A new 5‐fluorouracil–naproxen conjugate is synthesized as a mutual prodrug for targeting cancer tissues. The structure of the target compound and their intermediate are characterized by their melting point, IR, <sup>1</sup>H NMR, <sup>13</sup>C NMR, and elemental microanalysis. The cytotoxic activity is preliminarily evaluated using nonsmall lung cancer CRL‐2049, human breast cancer CAL‐51, and one type of normal cell line; rat embryo fibroblast cell line. The synthesized compound shows a good cytotoxic effect at the cancer cell and no significant effect at rat embryo fibroblast cell line.</p>
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Publication Date
Sun Jun 21 2020
Journal Name
Baghdad Science Journal
Synthesis of Carbon Nano Rods from Plastic Waste (PP) Using MgO AS A Catalyst
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    In this research, CNRs have been synthesized using pyrolysis of plastic waste(pp) at 1000 ° C for one hour in a closed reactor made from stainless steel, using magnesium oxide (MgO) as a catalyst. The resultant carbon nano rods were purified and characterized using energy dispersive X-ray spectroscopy (EDX), X-ray powder diffraction (XRD). The surface characteristics of carbon rods were observed with the Field emission scanning electron microscopy (FESEM). The carbon was evenly spread and had the highest concentration from SEM-EDX characterization. The results of XRD and FESEM have shown that carbon Nano rods (CNRs) were present in Nano figures, synthesized at 1000 ° C and with pyrolysis temperature 400° C. One of t

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Publication Date
Wed Mar 07 2018
Journal Name
Liquid Crystals
Synthesis and mesomorphism behaviour of chalcones and pyrazoles type compounds as photo-luminescent materials
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Publication Date
Mon Dec 30 2019
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Synthesis and Characterization of Nano Y Zeolite Using MWCNT as Media for Crystal Growth
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   The present research was conducted to synthesis Y-Zeolite by sol-gel technique using MWCNT (multiwalled carbon nanotubes) as crystallization medium to get a narrow range of particle size distribution with small average size compared with ordinary methods. The phase pattern, chemical structure, particle size, and surface area were detected by XRD, FTIR, BET and AFM, respectively. Results shown that the average size of Zeolite with and without using MWCNT were (92.39) nm and (55.17) nm respectively .Particle size range reduced from (150-55) nm to (130-30) nm. The surface area enhanced to be (558) m2/g with slightly large pore volume (0.231) km3/g was obtained. Meanwhile, degree of crystallization decrease

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Publication Date
Sun Feb 25 2018
Journal Name
Oriental Journal Of Chemistry
Synthesis and Study of Modified Polyvinyl Alcohol Containing Amino acid moieties as Anticancer Agent
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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
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
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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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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