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Synthesis and Preliminary Pharmacological Evaluation of Esters and Amides Derivatives of Naproxen as Potential Anti-Inflammatory Agents
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4-chloro and 4- nitro substituted phenol and aniline incorporated to a carboxylic group of naproxen a well-known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were synthesized for evaluation as  a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of these compounds (I-IV) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (2.5 mg/Kg) of naproxen. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, compounds I and IV might show higher effect comparable to that of naproxen and to that of compounds II & III which may attribute to the higher effect of nitro group than chloride group. The results of this study indicate that esterification and amidation of naproxen with selected pharmacophoric groups enhance or maintain its anti-inflammatory activity.    

 Keywords: anti-inflammatory; naproxen derivatives.

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Publication Date
Mon Aug 27 2018
Journal Name
Oriental Journal Of Chemistry
Synthesis, Characterization and Antibacterial Activity of Carbamate Derivatives of Isatin
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In search of novel antibacterial agent, a series of new isatin derivatives (3a-d) have been synthesized by condensation isatin (2,3-indolinendione) with piperidine (hexahydropyridine), hydrazine hydrate and Boc-amino acids respectively. Compounds synthesized have been characterized by IR spectroscopy and elemental analysis. In addition, the in vitro antibacterial properties have been tested against E. coli, P. aeruginosa, and Bacillus cereus, S. aureus by employing the well diffusion technique. A majority of the synthesized compounds were showing good antibacterial activity and from comparisons of the compounds, compound 3d has been determined to be the most active compound.

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Publication Date
Sat Feb 01 2025
Journal Name
Advanced Journal Of Chemistry, Section A
Synthesis and Characterization of Heterocyclic Derivatives to Evaluate their Efficiency as Corrosion Inhibitors for Carbon Steel in Saline Medium
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This work includes preparation of Az, Qz, and Tz derivatives from the reaction of Schiff base (Sb) derivative with anthranilic acid, chloroacetyl chloride, and sodium azide, as well as, the characterization via FT-IR, 1H-NMR, and 13CNMR. The anticorrosion inhibition of these compounds was studied and the measurements of carbon steel (CS) corrosion in sodium chloride solution 3.5% (blank) and inhibitor in solutions were calculated at a temperature range of 293-323 K by the technique of electrochemical polarization. In addition, some thermodynamic and kinetic activation parameters for inhibitor and blank solutions (Ea⋇, ΔH⋇, ΔS⋇, and ΔG⋇) were determined. The results showed high inhibition efficacy for all the prepared compounds,

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Publication Date
Thu Apr 11 2019
Journal Name
Scientific Reports
Small-Molecule Ferroptotic Agents with Potential to Selectively Target Cancer Stem Cells
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Abstract<p>Effective management of advanced cancer requires systemic treatment including small molecules that target unique features of aggressive tumor cells. At the same time, tumors are heterogeneous and current evidence suggests that a subpopulation of tumor cells, called tumor initiating or cancer stem cells, are responsible for metastatic dissemination, tumor relapse and possibly drug resistance. Classical apoptotic drugs are less effective against this critical subpopulation. In the course of generating a library of open-chain epothilones, we discovered a new class of small molecule anticancer agents that has no effect on tubulin but instead kills selected cancer cell lines by harnessing reactive oxygen </p> ... Show More
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Publication Date
Mon Oct 01 2018
Journal Name
European Journal Of Dentistry
The anti-inflammatory effect of the platelet-rich plasma in the periodontal pocket
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ABSTRACT<p> Objective: Chronic periodontitis (CP) is a common inflammatory disease that causes destruction to the supporting tissues of the teeth. Many treatment modalities tried to stop the disease progression. Platelet-rich plasma (PRP) is one of the regenerative methods that used in adjunct to conventional periodontal treatment. The aim of this study was to evaluate the anti-inflammatory effect of PRP by monitoring the lymphocyte count before and after its application to the periodontal pocket. Materials and Methods: Twenty patients, with CP and a pocket depth equal to or deeper than 4 mm, subjected to scaling, root planing, and PRP injection into the pocket. The lymphocyte count measured before an</p> ... Show More
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Publication Date
Sat Jun 18 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Development of novel paracetamol/naproxen co-crystals with an improvement in naproxen solubility.
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Co-crystals are new solid forms of drugs that could resolve more than one problem associated with drugs formulations like solubility, stability, bioavailability, mechanical and tableting properties. A preliminary theoretical study for estimating the possible bonding between the co-crystal components (paracetamol and naproxen) was performed using the ChemOffice program. The results revealed a high possibility for bonding between paracetamol and naproxen and indicated the ability of molecular mechanics study to predict the co-crystal design.

       In this work, four different methods were used for the preparation of three different ratios 1:1, 2:1, and 1:2 of paracetamol:naproxen co-crystals. The four

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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Dose-dependent Anti-inflammatory Effect of Silymarin in Experimental Animal Model of Acute Inflammation
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Silymarin, a flavolignans from seeds of ‘milk thistle’ “Silybum marianum” has been widely used from ancient times because of its excellent hepatoprotective action. It has been used clinically to treat liver disorders including acute and chronic viral hepatitis, toxin/drug-induced hepatitis and cirrhosis and alcoholic liver disease. The efficacy and dose-response effect of silymarin (125, 250 and 500 mg/kg) were assessed using egg albumin-induced paw edema in rats as a model of acute inflammation. In this model, 56 rats were used and allocated into 7 subgroups each containing 8 rats. All treatments were given intraperitonealy 30 minutes before induction of inflammation by egg albumin and then the increase

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Publication Date
Thu May 01 2025
Journal Name
Iraqi Journal Of Science
Synthesis and characterization of some 2-sulphanyl benzimidazole derivatives and study of effect as corrosion inhibitors for carbon steel in sulfuric acid solution
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This research involves the synthesis of some sulphanyl benzimidazole derivatives (Ia-c), which were prepared from reaction of 2-mercaptobenzimidazole substituted benzyl halide, and structures were identified by spectral methods[FTIR, 1H-NMR and 13C-NMR].These compounds were investigated as corrosion inhibitors for carbon steel in 1M H2SO4 solution using weight loss, potentiostatic polarization methods; obtained results showed that the sulphanyl benzimidazole derivatives retard both cathodic and anodic reactions in acidic media, by virtue of adsorption on the carbon steel surface. This adsorption obeyed Langmuir’s adsorption isotherm. The inhibition efficiency of (Ia-c) ranging between (65-92) %. By using different Ib derivative conc

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Publication Date
Tue Apr 30 2024
Journal Name
Iraqi Journal Of Science
Synthesis and Characterization of some new heterocyclic derivatives from aromatic carbonyl ‎compounds and carboxylic acids with Evaluation some of them for biological activity
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     In this research investigation, a total of eighteen diverse tetra- and penta-lateral cyclic compounds were synthesized. These included 1,3,4-thiadiazole, thiazolidin-4-one (via an alternative method), 1,2,4-triazole, carbothioamide, thiazole-4-one, azetidin-2-one, and oxazole. The synthesis procedure entailed a sequence of reactions. The thiazolidine-4-one 1 was obtained by reaction p-aminobenzoic acid with thiosemicarbazide, followed by treatment with p-tolualdehyde to produce Schiff base 2. Reaction Schiff base 2 with mercaptoacetic acid in dry benzene was carried out to produce thiazolidine-4-one 3. In another synthesis pathway, the esterification of p-nitro benzoic acid with ethanol in the presence of sulfuric acid was

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Publication Date
Tue Oct 22 2019
Journal Name
Scientia Pharmaceutica
Design, Synthesis, and Docking Study of Acyl Thiourea Derivatives as Possible Histone Deacetylase Inhibitors with a Novel Zinc Binding Group
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Histone deacetylase inhibitors with zinc binding groups often exhibit drawbacks like non-selectivity or toxic effects. Thus, there are continuous efforts to modify the currently available inhibitors or to discover new derivatives to overcome these problems. One approach is to synthesize new compounds with novel zinc binding groups. The present study describes the utilization of acyl thiourea functionality, known to possess the ability to complex with metals, to be a novel zinc binding group incorporated into the designed histone deacetylase inhibitors. N-adipoyl monoanilide thiourea (4) and N-pimeloyl monoanilide thiourea (5) have been synthesized and characterized successfully. They showed inhibition of growth of human colon adenoc

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Publication Date
Sun Dec 04 2016
Journal Name
Baghdad Science Journal
Extraction of Iraqi Jasminumsambac (L.)Oil and Study It?s Effect as Antioxidant Agents
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Key words:Jasminumsambac, Volatile oil, Antioxidant.

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