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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
Thu Sep 26 2019
Journal Name
Journal Of Pharmaceutical Research International
Synthesis and identification of novel 2-thioxoimidazolidin-4-one derivatives containing azo and ester groups
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The compounds 3-[4̄-(4˭-methoxybenzoyloxy) benzylideneamino]-2-thioxo-imidazolidine-4-one(3)aand 4-(1-(5-oxo- 2-thioxoimidazolidin-1-ylimino)ethyl)phenyl acetate(3)b were prepared from the reaction of aromatic aldehyde or ketone(1)a,bwith thiosemicarbazide to give aryl thiosemicarbazones(2)a,b ,followed by cyclization with ethylchloroacetate in the presence of fused sodium acetate. Treatment the compounds(3)a,bwith 4- hydroxybenzenediazoniumchloride yielded the correspondings4-((4-((4-hydroxyphenyl)diazenyl)-5-oxo-2- thioxoimidazolidin-1-ylimino)methyl)phenyl 4-methoxybenzoate(4)aand4-(1-(4-((4-hydroxyphenyl)diazenyl)-5-oxo-2- thioxoimidazolidin-1-ylimino)ethyl)phenyl acetate(4)b.The new 2-thioxo-imidazolidin-4-one with esters (5-7)a,b sy

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Publication Date
Mon Jul 04 2022
Journal Name
Al Mustansiriyah Journal Of Pharmaceutical Sciences
Bis-Schiff Bases of Isatin Derivatives Synthesis, and their Biological Activities: A Review
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Isatin is a heterocyclic molecule that belongs to one of the most important classes of organic compounds known as indolines. Isatin, isatin analogs, and their Schiff bases have recently attracted a lot of attention in medicinal chemistry. Isatin, itself, shows various biological activities such as antiviral, anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, and anticonvulsant. Bis- Schiff bases containing isatin moiety have been known to possess a wide spectrum of pharmacological activities. This review offers up-to-date information on the most active isatin bis-Schiff bases, which would include anticancer, antimicrobial, antiviral, anticonvulsant, anti-inflammatory, and analgesic activities. These observations c

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Publication Date
Thu Jun 29 2023
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Synthesis of Novel Porphyrin Derivatives and Investigate their Application in Sensitized Solar Cells
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Solar energy has significant advantages compared to conventional sources such as coal and natural gas, including no emissions, no need for fuel, and the potential for installation in a wide range of locations with access to sunlight. In this investigation, heterocyclic derivatives were synthesized from several porphyrin derivatives (4,4',4",4"'-(porphyrin-5,10,15,20-tetrayl) tetra benzoic acid) compound (3), obtained by reaction Pyrrole with 4-formyl benzoic acid. Subsequently, porphyrin derivative-component amides 5a, 5b, and 5c were produced by reacting compound (3) with amine derivatives at a 1:4 molar ratio. These derivatives exhibited varying sensitivities for utilization in solar cells, with compound 5a displaying the highest power

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Publication Date
Thu Jul 01 2021
Journal Name
Eurasian Chemical Communications
Synthesis of new heterocyclic derivatives from 2-furyl methanethiol and study their applications
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In this research, cyclic compounds derived from 2- furfural mercaptan (oxazole, triazoles) were synthesized, and their biological efficacy was measured and compared with standard drugs. Also, their effectiveness as anti-oxidant was measured and compared with ascorbic acid as a standard substance. Some of the synthesized compounds were deduced with good efficacy. © 2021 Sami Publishing Company. All rights reserved

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Publication Date
Sat Jan 01 2022
Journal Name
Journal Of Pharmaceutical Negative Results
Synthesis, Characterization and Study Electrical Conductivity of New Poly Thiadizole Derivatives, Silica Nanocomposites
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Heterocyclic polymers / silica nanocomposite one of important materials because of excellent properties such as thermal , electrical , and mechanical properties , so that hybrid nanomaterial are widely used in many fields, in this paper nanocomposite had prepared by modification of silica nanoparticals by using acrylic acid and functionalized the surface of nanoparticles, and using free Radical polymerization by AIBN as initiators and anhydrous toluene as solvent to polymerize functionalize silica nanoparticles with heterocyclic monomers to prepare heterocylic polymers / silica nanocomposite and study electrical conductivity , The nanocomposite which had prepared characterized by many analysis technique to study thermal properties such

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Publication Date
Mon Jul 04 2022
Journal Name
Al Mustansiriyah Journal Of Pharmaceutical Sciences
Bis-Schiff Bases of Isatin Derivatives Synthesis, and their Biological Activities: A Review
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Isatin is a heterocyclic molecule that belongs to one of the most important classes of organic compounds known as indolines. Isatin, isatin analogs, and their Schiff bases have recently attracted a lot of attention in medicinal chemistry. Isatin, itself, shows various biological activities such as antiviral, anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, and anticonvulsant. Bis- Schiff bases containing isatin moiety have been known to possess a wide spectrum of pharmacological activities. This review offers up-to-date information on the most active isatin bis-Schiff bases, which would include anticancer, antimicrobial, antiviral, anticonvulsant, anti-inflammatory, and analgesic activities. These observations c

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Publication Date
Wed Apr 01 2020
Journal Name
International Journal Of Pharmaceutical Research
Synthesis, Characterization, Study the Toxicity and Anticancer Activity of N,O-Chitosan Derivatives
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Publication Date
Tue Sep 01 2020
Journal Name
Molecular Crystals And Liquid Crystals
Synthesis and liquid crystalline behavior of some twin compounds derived from quinolone derivatives
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Publication Date
Wed Sep 14 2016
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of Systemic C-reactive Protein as a Systemic Inflammatory Marker in the Blood for Patients Undergoing Minor Oral Surgical Procedures
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Background: C-reactive protein (CRP) is an acute phase protein that its plasma levels increase after trauma or surgery so it is used as an indicator for the level of inflammation after surgery. The objective of this study is to investigate pre- and post-operative levels of CRP in three types of oral surgical interventions (Apicoectomy, Impaction, and Impacted teeth exposure). Materials and Methods: A total number of (48) healthy individuals aged (20-60) years who needed oral surgical intervention for either (removal of impacted third molars, exposure of an impacted canine, or Apicoectomy). A 4ml venous blood was obtained from each patient at two occasions (pre-operatively at the day of operation and post-operatively after 48 hours), then ce

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Publication Date
Tue Jul 01 2008
Journal Name
D
Synthesis and Identification of Some New Derivatives of Schiff bases Compounds and study their Biological activity
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A new series of Schiff bases compounds , containing an azomethine linkage was synthesized and expected to be biologically active .The structures of these compounds were identified by IR , Uv/vis spectra , melting points and followed by T.L.C.The biological activity of these compounds was studied