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Synthesize of New Ibuprofen and Naproxen Sulphonamide Conjugate with Anti-Inflammatory Study and Molecular Docking Study
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Non-steroidal anti-inflammatory drugs (NSAIDs) contain free –COOH which thought to be responsible for the GI irritation associated with all traditional NSAIDs. The esterification of this group is one of an approach to ultimate aim for reduce the gastric irritation; so in this study we synthesized and preliminarily evaluated new ester compounds as new analogues with expected selectivity toward COX-2 enzyme. Synthetic procedures have been successfully developed for the generation of the target compounds (III a and b). The synthetic approach involved multi-steps procedures which include: Synthesis of 4-hydroxy benzene sulphonamide ( I b ), synthesis of Naproxen and Ibuprofen acyl chloride and then reacting them with 4-hydroxy benzene sulphonamide to form final compounds ( III a-b) .The structures of these compounds were identified and characterized using (TLC), infrared spectroscopy (FT-IR), 1H NMR data and microanalysis (CHN).Pharmacological study as anti-inflammatory activities for the final compounds were studied in rats by induced edema type of inflammation. Moreover, the results of a docking study of compounds III a-b into the COX-2 binding site revealed that its mechanism was possibly similar to that of naproxen, a COX-2 inhibitor. The effect of them on COX-2 antibody was showed it could significantly inhibit COX-2 activity.

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Publication Date
Mon Jan 10 2022
Journal Name
Journal Of Biomimetics, Biomaterials And Biomedical Engineering
Synthesis, Molecular Modeling, DNA Damage Interaction, and Antioxidant Potential of Hesperidin Loaded on Gold Nanoparticles
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The flavonoglycone hesperidin is recognized as a potent anti-inflammatory, anticancer, and antioxidant agent. However, its poor bioavailability is a crucial bottleneck regarding its therapeutic activity. Gold nanoparticles are widely used in drug delivery because of its unique properties that differ from bulk metal. Hesperidin loaded gold nanoparticles were successfully prepared to enhance its stability and bioactive potential, as well as to minimize the problems associated with its absorption. The free radical scavenging activities of hesperidin, gold nanoparticles, and hesperidin loaded gold nanoparticles were compared with that of Vitamin C and subsequently evaluated in vitro using 2,2-diphenyl-1-picrylhydrazyl assay. The antioxi

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Publication Date
Sun Aug 28 2016
Journal Name
World Journal Of Pharmacy And Pharmaceutical Sciences
AN INSIGHT ON THE IDENTIFICATION OF CANCER STEM CELLS USING NOVEL IMMUNOLOGICAL AND MOLECULAR STRATEGIES
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Cancer stem cells (CSCs) are defined as a population of cells present in tumours, which can undergo self-renewal and differentiation. Identification and isolation of these CSCs using putative surface markers have been a priority of research in cancer. With this background we selected pancreatic normal and tumor cells for this study and passaged them into animal tissue culture medium. Further staining was done using alkaline phosphatase and heamatoxilin staining. Blue to purple colored zones in undifferentiated pluripotent stem cells and clear coloration in the chromatin material indicated pancreatic cells. Further studies on the cell surface marker CD 44 were done using ELISA. For this, the protein was extracted from cultivated normal and t

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Publication Date
Thu Aug 08 2024
Journal Name
New Materials, Compounds And Applications
MOLECULAR MODELLING AND THEORETICAL DESIGN OF NOVEL NIRMATRELVIR DERIVATIVES AS SARS-COV-2 ENTRY INHIBITORS
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The pandemic SARS-CoV-2 is highly transmittable with its proliferation among nations. This study aims to design and exploring the efficacy of novel nirmatrelvir derivatives as SARS entry inhibitors by adapting a molecular modeling approach combined with theoretical design. The study focuses on the preparation of these derivatives and understanding their effectiveness, with a special focus on their binding affinity to the S protein, which is pivotal for the virus’s access to the host cell. Considering molecular docking aspects in the scope of a study on nirmatrelvir derivatives and S protein, dynamics simulations with 25 nanoseconds of their binding are explored. The study shows that these derivatives might work as effective antivi

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Publication Date
Tue Mar 05 2024
Journal Name
International Journal Of Science And Research (ijsr)
Evaluation of Adherence to Methotrexate in a Sample of Iraqi Patients with Rheumatoid Arthritis Receiving Anti - TNF Medications
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Publication Date
Wed Dec 01 2021
Journal Name
Journal Of Physics: Conference Series
Analytical Study of the Royal-Jelly Effect on Sperms Morphological Characteristics and some Liver Function Parameters and their Correlation with some Antioxidants in Male Albino Rats Treated with Pregabalin Drug
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Abstract<p>In recent years, the consideration of natural products as anti-inflammatory and antioxidative treatments has more interested worldwide. Moreover, natural products are easily obtained and are relatively safe the Royal jelly (RJ) is one of them. The current study was carried to evaluate the effects of pregabalin (PGB) on physiological activity of sperms, reproductive hormones assay and some biochemical analysis. Forty (40) male albino rats (10-weeks-old) were divided into four groups (10 rats each): G1 (treated with PGB drug, 150 mg/kg B.wt (Lyrica-Pfizer-Pharmaceutical Industries), G2 (treated with RJ 1g/kg), G3 (treated with PGB drug and RJ together), and G4 control treated with norma</p> ... Show More
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Publication Date
Mon Nov 21 2022
Journal Name
Al-rafidain Journal Of Medical Sciences ( Issn: 2789-3219 )
Nanotechnology at the Molecular Level
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Materials with external dimensions of one or more nanometers are referred to as nanomaterials. These structures result from a number of manufacturing processes. They are used in many industries, including pharmaceuticals, which is the most significant one. Numerous variables, including size, shape, surface morphology, crystallinity, solubility, etc., affect physical properties. While new physical and chemical processes are being created constantly, the biological method is the ideal strategy for synthesizing nanoparticles since it is straightforward, safe, and economical. Different kinds of nanoparticles can be metabolically synthesized by a wide variety of biological sources, including plants, bacteria, fungi, and yeast. There are

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Publication Date
Tue Sep 01 2020
Journal Name
Biochemical And Cellular Archives
SYNTHESIS, SPECTRAL AND THERMAL CHARACTERIZATION OF NI(II), CU(II) AND ZN(II) COMPLEXES WITH NEW LIGAND TOWARDS POTENTIAL BIOLOGICAL APPLICATION
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Series of new complexes of the type [M2 (L)Cl4 ] are prepared from the new ligand[N1 ,N4 -bis(benzo[d]thiazol-2- yl)succinamide (L) derived from ethan-1,2-dicarbonyl chloride and 2-aminobenzothiozole,where, M= Ni(ii), Cu(ii) and Zn(ii) alsocomplexes of mix-ligands, the type [M(L)(8-HQ)]Cl, where, M = Ni(ii), Cu(ii) and Zn(ii),8-HQ= 8-Hydroxyquinoline. Chemical forms are obtained from their 1 H, 13CNMR, Mass spectra (for (L)), FT-IR and U.V spectrum, melting point, molar conduct.Using flame (AA), % M is determined in the complexes.The content of C, H, N and S in the (L) and its complexes was specified. Magnetic susceptibility and thermal analysis (TGA) of prepared compounds were measured.The propose geometry for all complexes[M2 (L)Cl4 ] wa

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Publication Date
Sun Jun 05 2022
Journal Name
Egyptian Journal Of Chemistry
Synthesis, Characterization, and Biological Activity of New Metal Ions Complexes with Schiff Base Derived from 2-Acetylthiophene and Isatin-3-Hydrazone
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This study describes the preparation of a new bidentate Schiff base derived from the condensation of Isatin-3-hydrazone with 2-acetylthiophene and the preparation of new series of complexes with a good yield. The prepared ligand was characterized by IR, UV-Vis, C.H.N.S elemental analysis, 1H and 13C NMR, LC-Mass spectroscopy, and physical measurements. Its complexes were analyzed by C.H.N.S elemental analyses, UV-Vis., FTIR, NMR, LC-Mass Spectra, atomic absorption spectroscopy, magnetic susceptibility, and conductivity measurements The results from spectroscopy and measurement studies showed that the ligand coordinated to the metal ion as a bidentate ligand via oxygen and nitrogen, forming an octahedral geometry around it. In vitro antimicr

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Publication Date
Tue Jun 15 2021
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of Mutual Prodrugs of Secnidazole and Ciprofloxacin and study Their Physicochemical Properties
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  Secnidazole was linked with ciprofloxacin as mutual prodrugs to get antibiotics with broader spectrum of activity, improved physicochemical properties and given by single dose to improve patient’s compliance. Furthermore, they provide structural modifications to overcome bacterial adaptation. The structures of the synthesized compounds were confirmed using FT-IR, mass spectrometry, elemental microanalysis (CHNO) and some physiochemical properties. This modification was led to an increase in Log P values for Mutual I (Log P 1.114) and Mutual II (Log P 1.97) compared with its values for Secnidazole (Log P -0.373) and ciprofloxacin (Log P -0.832). The solubility of prodrugs had been determined in different media, Mutual II showed 1

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Publication Date
Thu Jun 01 2023
Journal Name
Baghdad Science Journal
Synthesis and Characterization of Some New Pyridine and Pyrimidine Derivatives and Studying Their Biological Activities
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Heterocyclic systems, which are essential in medicinal chemistry due to their promising cytotoxic activity, are one of the most important families of organic molecules found in nature or produced in the laboratory. As a result of coupling N-(4-nitrophenyl)-3-oxo-butanamide (3) using thiourea, indole-3-carboxaldehyde, or piperonal, the pyrimidine derivatives (5a and 5b) were produced. Furthermore, pyrimidine 9 was synthesized by reacting thiophene-2-carboxaldehyde with ethyl cyanoacetate and urea with potassium carbonate as a catalyst. The chalcones 11a and 11b were synthesized by reacting equal molar quantities of 1-naphthaldehy

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