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bijps-489
Synthesis and Preliminary Pharmacological Evaluation of New Analogues of Diclofenac as Potential Anti-inflammatory Agents
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         A group of amine derivatives [4-aminobenzenesulfonamide derivatives, 2-aminopyridine and 2-aminothiazole] incorporated to α-carbon of diclofenac a well known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were designed and synthesized for evaluation as  a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of the selected final compounds (9, 12 and 13) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (3 mg/Kg) of diclofenac sodium. All tested compounds  produced a significant reduction  in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the 4-aminobenzenesulfonamide derivative (compound 9) exhibited superior anti-inflammatory activity compared to diclofenac sodium at times 180-300 minutes with the same onset of action. The results of this study indicate that the incorporation of the selected aromatic amino groups in to diclofenac maintain its anti-inflammatory activity.                                                                                                                             

Key words: amine derivatives, anti-inflammatory, diclofenac derivatives, COX-2 selectivity.                                                                                                 

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Publication Date
Sat Dec 29 2018
Journal Name
Journal Of Global Pharma Technology
Synthesis, Characterization and Study Biological Activity of Some New Compounds Derived From Phthalic Anhydride
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In this research , phthallic anhydride ring is opened with 4-methyl aniline and acetone as a solvent to results the compound [I] that reacted with dimethyl sulphate and anhydrous sodium carbonate formation to phathalate ester [II], while the acid hydrazide compound [III], was obtained from mixed the compound [II]with hydrazine hydrate, Synthesis four type of shiff bases[IV]a-d was synthesized from the reaction of acid hydrazide [III] with aromatic aldehyde or ketone , when reacted Shiff bases with phthalic anhydride or naphthalicanhydride,I get eight derivatives of oxazepine [V]a-d , [VI]a-d. The bacterial activity of the new compounds studied by four species of bacteria: Esherichia Coli, Enterobactecloacae (Gram negative) and staphylococcu

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Publication Date
Wed Oct 07 2020
Journal Name
Indian Journal Of Forensic Medicine & Toxicology
Synthesis and Study the Biological Activity of New Heterocyclic Compounds Derived From Hydrazide Derivatives
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Publication Date
Fri Jun 25 2021
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization, Thermal and Biological Study of New Organic Compound with Some Metal Complexes
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A new set of metal complexes by the general formula [M(P)2(H2O)2]Cl2 has been prepared through the interaction of the new Ligand [N1, N4-bis(4-methoxyphenyl)succinamide] (P) derived from succinyl chloride with p-anisidine with the transition metal ions [Cu(II), Mn(II), Cd(II), Co(II) and Ni(II)]. Compounds diagnosed by TGA, 1 H, 13CNMR and Mass spectra (for (P)), Fourier-transform infrared and Electronic spectrum, Magnetic measurement, molar conduct, (%M, %C, %H, %N). These measurements indicate that (P) is associated with the metal ion in a bi-dentate fashion by nitrogen atoms (the amide group), and the octahedral composition of these complexes is suggested. Staphylococcus Aureus (+) and Escherichia Coli (–) were studied for the antibact

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Publication Date
Sat Dec 01 2018
Journal Name
Journal Of Pharmaceutical Sciences And Research
Synthesis and biological activity of new esters derived from D-fructose-containing isoxazole moiety
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Background: Isoxazoles are an important class of five-membered unsaturated heterocyclic compounds. They show several applications in diverse areas such as pharmaceuticals, agrochemistry and industry. Isoxazoles are also found in natural sources showing insecticidal, plant growth regulation and pigment functions. Current study was conducted for synthesis of twenty five new Isoxazole derivatives and to evaluate the in vitro antibacterial activities of these derivatives. Methods: Benzaldoxime and their substituted [I] ae were prepared via addition-elimination reactions between aromatic aldehyde and hydroxylamine hydrochloride. In a second step, para-or meta-substituted benzaldoximes [I] ae were reacted with N-chlorosucceinimide in DMF to yield

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Publication Date
Thu Jun 27 2019
Journal Name
Molecular Crystals And Liquid Cryst
A New Series of Triazine-core Based Mesogenic Derivatives: Synthesis, Characterization and Mesomorphic Study
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The synthesis, characterization and mesomorphic properties of two new series of triazine-core based liquid crystals have been investigated. The amino triazine derivatives were characterized by elemental analysis, Fourier transforms infrared (FTIR), 1HNMR and mass spectroscopy. The liquid crystalline properties of these compounds were examined by differential scanning calorimetry (DSC) and polarizing optical microscopy (POM). DSC and POM confirmed nematic (N) and columnar mesophase textures of the materials. The formation of mesomorphic properties was found to be dependent on the number of methylene unit in alkoxy side chains.

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Publication Date
Tue Feb 12 2013
Journal Name
International Journal Of Engineering Sciences And Research Technology
Synthesis, Characterization of New Azo Compounds and Studies Effect on the Ach Enzyme(Invitro)
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Three azo compounds were synthesized in two different methods, and characterized by FT-IR, HNMR andVis) spectra, melting points were determined. The inhibitory effects of prepared compounds on the activity of human serum cholinesterase have been studied in vitro. Different concentrations of study the type of inhibition. The results form line weaver-Burk plot indicated that the inhibitor type was noncompetitive with a range (33.12-78.99%).

Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New Mannich Bases Derived from 7-hydroxy-4-methyl Coumarin
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Coumarin is a natural substance isolated from different plants. It belonges to a group of benzobyrones which consists of a benzene ring joined to a pyrone nucleus. In the present research, a new series of coumarin derivatives were formed. Compound (1) (7-hydroxy-4-methyl Coumarin) was converted into 4-methylquinolin-2(H) derivative (2) by reaction with acetamide, and then reaction of (2) with thiosemicarbazide in ethanol leads to the synthesize of hydrazincarbothioamide derivative (3).The reaction of (3) with ethylchloroacetate in presence of sodium acetate leads to closure ring to get [(1-(5-oxo-2-thioxoimidazolidin-1-ylimino) ethyl)]quinolin-2(1H)-one (4). Mannich bases were prepared through the reaction of (4) with primary

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Publication Date
Mon Jun 27 2022
Journal Name
. J Pharm Negative Results
Synthesis, Antioxidant, antibacterial and docking structure of new dihydro-pyrimidine derivatives containing multi phenol
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Newly series of 6,6’-((2-(Aryl)dihydropyrimidine-1,3(2H,4H)-diyl)bis(methylene))bis(2-methoxy phenol) (3a-i) were synthesized from cyclization of 6,6’-((propane-1,3-diylbis (azanediyl)) bis(methylene)) bis(2-methoxyphenol) with several aryl aldehyde in the presence of acetic acid. The newly compounds characterized from their IR, NMR and EIMs spectra. The antioxidant capacity of these compounds screened by utilizing DPPH and FRAP assays. Compounds 3g and 3i exhibited significant antioxidant capability in both assays. Docking study for these compounds as a potential inhibitors of gyrase enzyme were carried out. Compound 3g exhibited significant inhibition with binding free energies (DG) higher than novobiocin. compounds 2, 3a, 3b, 3

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Publication Date
Sun Mar 13 2011
Journal Name
Baghdad Science Journal
Effect of Diclofenac (Voltaren) in histological structure of kidney in male Rabbits (Oryctolagus cuniculus )
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This study was designed to know the effect of Diclofenac sodium (voltaren) drug on the histological composition of kidney in domestic rabbits . Twelve adult males with (1.4) kg weight . The first group of animals administrated orally by 1 ml of Voltaren with 6 mg/kg , while the second group with (1) ml of distal water (as control group ) . the administrated continue for (60) days sequentially. The treatment with voltaren showed pathological cases in tissues and cells of kidney including necrosis, infilteration ,congestion in blood vessels edema.Also epithelial separation in kidney tubules in comparison with control group Conclusion from the above results, revealed that voltaren had negative effects on the kidn

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Publication Date
Wed Jan 29 2020
Journal Name
Advances In Rheumatology
Neutrophil/lymphocyte and platelet/lymphocyte ratios as potential markers of disease activity in patients with Ankylosing spondylitis: a case-control study
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Abstract<sec> <title>Background

The neutrophil/ lymphocyte ratio (NLR) and platelet/lymphocyte ratio (PLR) have the potential to be inflammatory markers that reflect the activity of many inflammatory diseases. The aim of this study was to evaluate the NLR and PLR as potential markers of disease activity in patients with ankylosing spondylitis.

Methods

The study involved 132 patients with ankylosing spondylitis and 81 healthy controls matched in terms of age and gender. Their sociodemographic data, disease activity scores using the Bath Ankylosing

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