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bijps-415
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
Thu Dec 15 2022
Journal Name
Bionatura
NDRG1 is being investigated as a possible bladder cancer biomarker in the Iraqi population.
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With 549,393 new cases recorded in 2018, bladder cancer is one of the most common malignancies worldwide. Urinary bladder cancer is the cause of about 3 percent of all new cancer diagnoses and 2.1 percent of all cancer deaths. This study aims to evaluate the efficiency of the N-myc downstream-regulated gene 1(NDRG1) as a biomarker for bladder cancer patients in the Iraqi population. One hundred individuals in the case-control study were enrolled and divided into two groups. The first group included 50 patients diagnosed with a bladder mass and investigated by undergoing cystoscopy examination for transurethral resection of bladder tumor (TURB). The second group included 50 healthy individuals who had normal bladder tissue. The resul

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Publication Date
Sat Jan 01 2022
Journal Name
Pharmacia
Synthesis, docking study, and structureactivity relationship of novel niflumic acid derivatives acting as anticancer agents by inhibiting VEGFR or EGFR tyrosine kinase activities
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Publication Date
Thu Jun 01 2023
Journal Name
Baghdad Science Journal
Batch and flow injection spectrophotometric methods for determination of Ceftazidime in pharmaceutical formulations
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It is generally accepted that there are two spectrophotometric techniques for quantifying ceftazidime (CFT) in bulk medications and pharmaceutical formulations.  The methods  are described as simple, sensitive, selective, accurate and efficient techniques. The first method used an alkaline medium to convert ceftazidime to its diazonium salt, which is then combined with the 1-Naphthol (1-NPT) and 2-Naphthol (2-NPT) reagents. The azo dye that was produced brown  and red in color with absorption intensities of ƛmax 585 and 545nm respectively. Beer's law was followed in terms of concentration ranging from  (3-40) µg .ml-1 For (CFT-1-NPT) and (CFT-2-NPT), the detection limits were 1.0096 and 0.8017 µg.ml-1, respec

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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Preparation and Identification of some new Pyrazolopyrin derivatives and their Polymerizations study
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Preparation and Identification of some new Pyrazolopyrin derivatives and their Polymerizations study

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Publication Date
Mon Feb 08 2016
Journal Name
Iraqi Journal Of Science,
Synthesis, Identification and Evaluation Biological Activity for Some New Triazole, Triazoline and Tetrazoline Derivatives From 2-Mercapto-3- phenyl-4(3H)Quinazolinone
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This research, involved synthesis of some new 1,2,3-triazoline and 1,2,3,4- tetrazole derivatives from antharanilic acid as starting material .The first step includes formation of 2-Mercapto-3-phenyl-4(3H)Quinazolinone (0) through reacted of anthranilic acid with phenylisothiocyanate in ethanol, then compound (0) reaction with chloro acetyl chloride in dimethyl foramamide (DMF) to prepare intermediate S-(α-chloroaceto-2-yl)-3-phenylquinazolin-4(3H)-one (1); compound (1) reacted with sodium azide to yield S-(α-azidoaceto-2-yl)-3-phenylquinazolin-4(3H)-one (2), while Schiff bases (3-10) were prepared from condensation of substituted primary aromatic amines with different aromatic aldehydes in absolute ethanol as a solvent. Compound (2)

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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)
Evaluation of Stability of Cefamandol and Ceftazidime with Clavulanic Acid Against Extended Spectrum ?- Lactamase
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The aim of this study is to evaluate in-vitro activity of Cefamandol (Cfm) and Ceftazidime (Cfz), in combination with Clavulanic acid (CA) against ten complicated multiresistant uropathogenic E.coli .One hundred clinical strains were isolated from patients with chronic urinary tract infections (UTIs), these isolates were identified by the Api identification systems. The antimicrobial susceptibility tests were determined by Kirby-Bauer method, all of them were sensitive to Imipenem (Imp). Ten strains were chosen for the present study, they were resistant to Ampicillin (Amp), Amoxicillin (Amo), Carbenicillin (Cb), Ticarcillin (Tic), Azlocillin (Azl), Amoxicillin\ Potassium Clavulanate {Augmentin(Amc)}, (Amo\CA), Ticarcillin\ Potas

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Publication Date
Mon Apr 15 2024
Journal Name
Al-rafidain Journal Of Medical Sciences ( Issn 2789-3219 )
Evaluation of the Wound-Healing Activity and Apoptotic Induction of New Quinazolinone Derivatives
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Background: Chemotherapeutic medication treatment for cancer is typically used in conjunction with other techniques as part of a routine regimen. It is well established that the capacity of different chemotherapeutic drugs to induce apoptosis is correlated with their anticancer efficacy. Quinazolinone-based drugs have demonstrated excellent responses from several cancer cell types. These substances have a lot of potential for use as building blocks in the creation of apoptosis inducers. Objective: To assess the new quinazolinone derivatives (M1 and M2) that were recently synthesized for their potential to halt wound healing and to use the acridine orange/propidium iodide (AO/PI) double stain to assess their capacity to induce apopto

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Publication Date
Tue Jan 21 2025
Journal Name
Applied Biochemistry And Biotechnology
Synthesis and characterization of new (Au, Ru, and Rh) ion complexes and evaluating their activity as anticancer and antioxidants
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Publication Date
Wed Jan 01 2020
Journal Name
Annals Of Tropical Medicine And Public Health
Synthesis and characterization of new phthalimide with 6- mercaptopurine or 2- aminothiazole conjugate used dithiocarbamate spacer as anticancer agents
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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
Synthesis of New Amide and ThioUrease Compounds.
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The reaction of some new Schiff bases ( 2-[(2-Amino – ethylimino)-methyl]-R , 2-({2-[(R-benzylidene)-amino]-ethylimino}-methyl)-R with Benzoyl chloride or Acetyl chloride were carried out. Subsequent reactions of these products N-(2-Amino-ethyl)-N-[Chloro-(R) –methyl]-benzamide or N-(2-{?-[chloro-(R) –methyl]-amino}-ethyl)-N-[chloro-(R) –methyl]- benzamide with thiourea afforded thioureas compounds. The synthesized compounds were confirmed by their IR,UV,spectra and C.H.N. analysis.

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