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Design and Synthesis of New Non-Steroidal Anti-inflammatory Agents with Expected Selectivity toward Cyclooxygenase-2 Inhibition

This study includes design and synthesis of new non-steroidal anti-inflammatory agents (NSAIDs) with expected cyclooxygenase-2 (COX-2) selective inhibition to achieve better activity and low gastric side effects. Two series of compounds have been designed and synthesized as potential NSAIDs,these  are:     Salicylamide derivatives (compounds 3,4,5 ) and Diflunisal derivatives (compounds 10&11). In vivo acute anti-inflammatory effect of one of the synthesized agents (compound 3)  was evaluated in the rat using egg-white induced paw edema model of inflammation. Preliminary pharmacological study revealed that compound 3 exhibited less anti-inflammatory effect  compared to that of aspirin after 120 and 210 minutes, which encourage the continuation of the search to demonstrate or identify the preliminary pharmacological activity for the  synthesized compounds and to identify their selectivity toward COX-2 isoenzymes.

Keywords:nonsteriodal anti-inflammatory drugs(NSAID),aspirin derivatives ,diflunisal, Cyclooxygenase -1(cox-1),cyclooxygenase-2(cox-2)

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Publication Date
Fri Jul 01 2022
Journal Name
Iraqi Journal Of Science
Synthesis and Characterization of Several New Succinimides Linked to Phenyl Azo Benzothiazole or Thiazole Moieties with Expected Biological Activity

In the present work, several new cyclic imides (succinimides) linked to benzothiazole or thiazole moieties through phenyl azo group were synthesized. Synthesis of the new imides was performed via multistep synthesis. The first step involved reaction of equimolar amounts of succinic anhydride and p-toluidine producing N-(4-tolyl) succinamic acid (1) which was dehydrated in the second step via treatment with acetic anhydride and anhydrous sodium acetate affording N-(4-tolyl)succinimide (2).
In the third step, substituted-2-aminobenzothiazoles were introduced in diazotization reaction with nitrous acid producing the corresponding diazonium salts and these inturn were introduced directly in coupling reaction with compound (2) affording th

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Publication Date
Tue Jun 05 2018
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Alpha Glucosidase Inhibition activity of new Phthalimide Derivatives

 Three of imide intermediate products  were synthesized by reacting of phthalic anhydride with glycine (2a), and tetrachloro phthalic anhydride with glycine , (S)-2-[(tert-Butoxycarbonyl)amino]-3-aminopropionic acid ( 2b,c)  respectively   in  dry toluene  with azeotropic removal of water using Dean- stark apparatus then carboxyl functional group activated by refluxing with  thionyl chloride, the resulted acid chloride (3a-c) were reacted with different amine (5-flourouracil, 4-chloroaniline, 4-bromoaniline, 2-amino thiazole, and pyrrolidine) (4a-e) , the   resulted products consider as

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Publication Date
Sun Sep 04 2016
Journal Name
Baghdad Science Journal
Synthesis and Characterization of Some New Pyrazoline and Isoxazoline Derivatives as Antibacterial Agents

In this paper some chalcones (C1-C8) are prepared based on the reaction of one mole of substituted acetophenone with one mole of substituted benzaldehydes in the presence of (40%) sodium hydroxide as a base. Pyrazolines (P1–P8) are prepared from the reaction of chalcones (C1-C8) with hydrazine hydrate. Isoxazoline (I1-I8) is prepared from the reaction of chalcones (C1-C8) with hydroxyl amine hydrochloride in the presence of (10%) sodium hydroxide as a base. These compounds are characterized by using various physical and spectral methods. The compounds are screened for their in vitro antibacterial activity using gram-positive bacteria and gram-negative bacteria. Several derivatives of pyrazolines and isoxazolines are produced well to moder

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Publication Date
Mon Jun 03 2019
Journal Name
Journal Of Global Pharma Technology
New Diquinazoline Derivatives: Synthesis and Evaluation of AntiBacterial Activi

Oxazine and quinazoline has a very important in organic chemistry especially in hetero cyclic fields. this research consist the preparation of 4H,4'H-2,2'-bibenzo[d][1,3]oxazine-4,4'-dione compound (1) from di acid chloride with 2-aminobenzoic acid in pyridine as solvent to give compound (2) 3,3'-diamino-2,2'- biquinazoline-4,4'(3H,3'H)-dione .compound 2 include free amino group .this compound was reacted with maleic and phthalic anhydride for synthesized of cyclic imide compounds (3,4).another reaction for compound 2 with some substituted aromatic aldehyde for prepared of some novel Schiff bases (5-9) contains quinazoline ring. compound 1 was treated with sulfathiazole and sulfadiazine for synthesized of sulfa compounds contains sulf

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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)
Effect of COX-2 Inhibitors Selectivity on Lipid Profile in Hyperlipidemic and Normolipidemic Type 2 Diabetics

Development of NSAIDS based on inhibiting cyclooxygenase activity. However, the different physiological consequences arrised by appearance of new drugs with different selectivity to COX-2 enzyme upon their administration with their relevant affects on some cardiovascular risk factors. To study the potential effects of relatively  diclofenac and highly specific  celecoxib COX-2 inhibitors on lipid profile and serum C-reactive protein in type 2 diabetes, whom have hyperlipidemia to be compared by their effects with normolipidemic patients. A total number of 34 type 2 diabetics (14 normolipidemics and 20 hyperlipidemics) treated with either diclofenac 100mg/day or celecoxib 200mg/day for eight weeks. Analysis  of results indi

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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis and characterization of new complexes of Co+2 , Ni+2 , Cu+2 and Zn+2 with (Sodium acetate thio ) ethylene ligands

This research involves the preparation of new ligands 1,1,2,2- tetrakis (sodium acetate thio)ethylene(L1) and 1,1,2- tris(sodiumacetatethio) ethylene(L2), through the reaction of disodium thioglycolate) with tetra chloro ethylene or tri chloro ethylene in (1:4) or (1:3) moler ratio . Homodinucliar complexes of general formlu [M2(L1)] and [M2(L2)ClH2O] , when M= Co(II), Ni(II), Cu (II) and Zn(II) also mono nuclear complexes of general formula [M(L2)] . The prepared complexes were characterized using spectral method (UV/Visible/ IR) , metal content analysis , magnetic and atomic measurements . The spectral and magnetic measurement indicats that some complexes have tetrahedral or square planar complexes environtment .

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Publication Date
Thu Apr 29 2021
Journal Name
Iraqi Journal Of Science
Synthesis and Characterization of Silver Nanoparticles Using Prodigiosin Pigment and Evaluation of Their Antibacterial and Anti-Inflammatory Activities

This study focused on the biological synthesis of silver nanoparticles (AgNPs), using prodigiosin pigment produced by Serratia marcescens. The effect of parameters such as pH, temperature, time, with various concentrations of silver nitrate (AgNO3) and prodigiosin on the synthesis of AgNPs were also studied.  Optimized results of the biosynthesis process revealed an increase in the intensity of Surface Plasmon Resonance (SPR) bands of nanoparticles with shifting at the wavelength of 400 nm. In addition, optimum synthesis of AgNPs was achieved at pH 12, temperature 55℃, and reaction time 24 h, with concentrations of prodigiosin, as a reducing agent, of 12.5 µg/ml and silver ion concentration of 1 mM. Measuremen

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Publication Date
Wed Jul 10 2024
Journal Name
Pharmacia
Molecular docking, ADMET, synthesis and evaluation of new indomethacin hydrazide derivatives as antibacterial agents

Bacterial infections pose an ongoing challenge due to resistance developed by infectious bacteria. So much research targeting designing new antibacterials is published annually. Our goal is to synthesize compounds that have given antibacterial activity according to molecular docking against the chosen target protein and that have acceptable ADMET properties that can be synthesized and used in the future. New 2-(5-methoxy-1-(4-chlorobenzene)-2-methyl-1H-indol-3-yl)acetohydrazide derivatives’ antibacterial efficacy against two common strains of Gram-negative and Gram-positive microorganisms has been developed, produced, and investigated. Sophisticated, modern analytical methods, including ATR-FTIR and 1H NMR spectroscopy, were used

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Publication Date
Sun Jan 03 2010
Journal Name
Journal Of The Faculty Of Medicine Baghdad
The Effect of Selectivity of Inhibitors to Cox-2 Enzyme on Hepatobiliary and Platelet Function in Patients with Osteoarthritis

Background: The development of non steroidal anti-inflammatory drugs (NSAIDs) was based principally on inhibiting cyclooxygenases (COX) activity. However, the identification of two
COX- isoforms (i.e., COX-1 and COX-2) with different physiological effects has led to the development of COX-2 specific NSAIDs, with fewer adverse effects than traditional NSAIDs.
Therefore, They are expected to produce anti-inflammatory activity with minimal adverse effects on GI mucosa, as well as, other structures and cells such as platelets.
The aim of this study is to evaluate the effect of selectivity of COX-2 inhibitors on many organs and systems function such as the hepatobiliary system, platelets function, as well as, seru

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Publication Date
Sun Oct 03 2010
Journal Name
Journal Of The Faculty Of Medicine Baghdad
Role of Pro- and Anti-Inflammatory Cytokines in Rheumatoid Arthritis: Correlation with Disease Activity.

Background: Rheumatoid arthritis (RA) is a chronic and debilitating autoimmune disease characterized by chronic inflammation with subsequent cartilage and bone destruction. Cytokines are  key mediators of inflammation and can be found in abundance both in the joint and blood of patients. This study was designed to evaluate the role of pro- and anti-inflammatory cytokines in pathogenesis of RA, as well as study the correlation among these cytokines.
Patients and methods: Forty patients with RA and thirty age-matched healthy controls were included in this study. Serum cytokines were measured by enzyme-linked immunosorbent assay.
Results: The serum levels of pro-inflammatory cytokines (IL-1α, IL-2, IL-6, IL-8

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