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bijps-531
Synthesis and Preliminary Pharmacological Study of Sulfonamide Conjugates with Ibuprofen and Indomethacin as New Anti-Inflammatory Agents
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          4-aminobenzenesulfonamide conjugates of ibuprofen (compound 10) and indomethacin (compound 11) have been designed and synthesized by the reaction of sulfanilamide (compound 7) with 2-(4-isobutylphenyl) propanoic acid (ibuprofen) and 2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetic acid (indomethacin) for the evaluation as potential anti-inflammatory agents with expected selectivity against COX-2 enzyme. In vivo acute anti-inflammatory activity of the synthesized final compounds (10 and 11) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (10mg/Kg) of ibuprofen and (2mg/kg) of indomethacin. The tested compounds produced significant reduction of the rat paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, compound (10) exhibited comparable anti-inflammatory activity to diclofenac (3mg/Kg) (reference group) while compound (11) exhibited less anti-inflammatory activity than diclofenac. The result of this study indicate that the incorporation of the 4-aminobenzenesulfonamide pharmacophore into ibuprofen and indomethacin maintained their anti-inflammatory activity & may increase their selectivity toward COX-2 enzyme which can be confirmed in future by assessing COX-2:COX-1 inhibitory ratio.

Key words: Cyclooxygenase; Anti-inflammatory activity; Ibuprofen; indomethacin; NSAIDs.

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Publication Date
Mon Jul 01 2019
Journal Name
Journal Of Global Pharma Technology
Synthesis and Characterization of Some New Pyrazole Derivatives‏
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This work contain many steps starting from esterification of isophthalic acid to yield diester compound [I] which was converted to their acid hydrazide [II], then the later compound reacted with ethylacetoacetate to yield pyrazol-5-one compound [III]. Afterword added acetyl chloride to give the compound [IV], the reaction of this compound with theiosemicarbazide led to produce a new carbothioamide compound [V], which was reacted with ethyl chloro acetate to yield the thioxoimidazolidin compound [VI]. The condensation reactions of this compound with different substituted aldehyde give new alkene derivatives [VII] ad. The synthesized compounds were characterized by melting points, FT-IR, 1H-NMR and Mass spectroscopy.

Publication Date
Sun Mar 06 2016
Journal Name
Baghdad Science Journal
Synthesis and Characterization of Some New Benzimidazole Derivatives
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In this paper the new starting material 2-(5-chloro-1H-benzo[d]imidazole-2-yl) aniline (1) was synthesized by the condensation reaction of 4-chloro-o-phenylenediamine and anthranilic acid .The new Mannich base derivatives were synthesized using formaldehyde and different secondary amines to synthesize a new set of benzimidazole derivatives(2-5). Also, the new Schiff-base derivatives (6-10) were synthesized from the reaction of compound (1) with various aromatic aldehydes and the closure-ring was done successfully using mercapto acetic acid to get the new thiazolidine derivatives(11-12).These new compounds were characterized using some physical techniques like:FT-IR Spectra and 1HNMR Spectra.

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Publication Date
Sun Dec 01 2013
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New Polyimide Contain Heterocyclic
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Novel heterocyclic polyimide 5(a,b) have been synthesized based on polyacrylic backbone. The synthetic route start with nucleophilic substitution of 2-amino, or 4-amino, pyridine 1(a,b) to the polyacryloyl chloride afforded poly substituted amide 2(a,b). Another nucleophilic substitution were carried with adipoyl chloride to form polyimide chloride 3(a,b). Treatment of 3(a,b) with hydrazine hydrate afforded acid hydrazide polyimide 4(a,b), which upon cyclocondensation with carbon disulfide gave the target heterocyclic polyimide. The synthesized compounds were identified by spectroscopic methods: FT-IR, 1H-NMR and 13C-NMR.

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Publication Date
Mon Jun 01 2020
Journal Name
Journal Of Pharmaceutical Sciences And Research
Synthesis and Biological Activity of New Imidazaldinone Derivatives
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A research include of synthesized five member ring, which has been synthesized by condensation of 2-(1-(4- hydroxyphenyl) ethylidene)hydrazine-1-carbothioamide[I] with α-chloro ethylacetate in sodium acetate (fused) to form ethyl 2-(4-(1-((4-oxo-2-thioxopyrrolidin-3-ylidene)hydrazono) ethyl)phenoxy)acetate [II]. After that reacted [II]with hydrazine hydrate to resulting compound [III]. Compound [III] was refluxed with 4-aminobenzoicacid in excess of phosphorus oxy chloride give compound [IV],the later compound [IV] interact with acetyl acetone or ethylacetoacetate give to pyrazole and pyrazoline derivatives[V],[VI]. While when reacted with different aromatic aldehydes and one ketone consistence Schiff base derivatives [VII]a-e . The FTIR a

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Publication Date
Thu Dec 29 2016
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of Some New 1,3Oxazepine Derivatives
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  In this study, Schiff's bases [S3,S4] were synthezied by condensation of N,N-dimethyl amino benzaldehyde with primary aromatic amine[N-(hydrazinyl methyl)benzamide]. These Sciff's bases were found to react with maleic anhydride and phthalic anhydride to give 1,3Oxazepine[S5,S6,S7,S8] in good yields.            The structures confired by m.p ,T.L.C.,FT.IR and 1H-NMR (of some of them).

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Publication Date
Tue May 12 2020
Journal Name
International Journal Of Pharmaceutical Research
Synthesis and Biological Activity of New Imidazaldinone Derivatives
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A research include of synthesized five member ring, which has been synthesized by condensation of 2-(1-(4- hydroxyphenyl) ethylidene)hydrazine-1-carbothioamide[I] with α-chloro ethylacetate in sodium acetate (fused) to form ethyl 2-(4-(1-((4-oxo-2-thioxopyrrolidin-3-ylidene)hydrazono) ethyl)phenoxy)acetate [II]. After that reacted [II]with hydrazine hydrate to resulting compound [III]. Compound [III] was refluxed with 4-aminobenzoicacid in excess of phosphorus oxy chloride give compound [IV],the later compound [IV] interact with acetyl acetone or ethylacetoacetate give to pyrazole and pyrazoline derivatives[V],[VI]. While when reacted with different aromatic aldehydes and one ketone consistence Schiff base derivatives [VII]a-e . The FTIR a

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Publication Date
Sat Sep 01 2018
Journal Name
Journal Of Global Pharma Technology
Synthesis and Characterization of Some New Pyrazole Derivatives
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This work contain many steps starting from esterification of isophthalic acid to yield diester compound [I] which was converted to their acid hydrazide [II], then the later compound reacted with ethylacetoacetate to yield pyrazol-5-one compound [III]. Afterword added acetyl chloride to give the compound [IV], thereaction of this compound with theiosemicarbazide ledto produce a new carbothioamide compound [V], Which was reacted with ethyl chloro acetate to yield thethioxoimidazolidin compound [VI]. The condensation reaction of this compound with different substituted aldehyde give new alkene derivatives[VII]a-d. The synthesized compounds were characterized by melting points , FT-IR ,1H-NMR and Mass spectroscopy .

Publication Date
Sun Dec 01 2019
Journal Name
Journal Of Medicinal And Chemical Sciences
Synthesis and Identification of New 2-Substituted-1,3,4-Oxadiazole Compounds from Creatinine and Study Their Antioxidant Activities
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Publication Date
Fri Dec 01 2017
Journal Name
Iraqi Postgraduate Medical Journal
The polycystic ovary syndrome as a cause of increase in inflammatory markers and metabolic risks
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BACKGROUND: Polycystic ovary syndrome(PCOS) is one of the most common endocrine disorder affecting women in reproductive age. No single etiologic factor fully accounts for the spectrum of abnormalities in the polycystic ovary syndrome. Different changes in hormonal, metabolism and the inflammatory markers as squealy of PCOS with adverse effect on the women life. OBJECTIVE: To study the relationship between polycystic ovary syndrome and levels of C-reactive protein, human interleukin and hormonal and metabolic alteration in women with PCOS PATIENTS AND METHODS: Thirty women with Polycystic Ovary syndrome (PCOS) and other thirty women without PCOS were included. Venous blood samples were taken in early follicular phase of menstrual cycle [day

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Publication Date
Tue Oct 01 2019
Journal Name
The Journal Of Immunology
AhR Activation Leads to Massive Mobilization of Myeloid-Derived Suppressor Cells with Immunosuppressive Activity through Regulation of CXCR2 and MicroRNA miR-150-5p and miR-543-3p That Target Anti-Inflammatory Genes
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Abstract<p>The compound 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), an environmental contaminant, is a potent ligand for aryl hydrocarbon receptor (AhR). In the current study, we made an exciting observation that naive C57BL/6 mice that were exposed i.p. to TCDD showed massive mobilization of myeloid-derived suppressor cells (MDSCs) in the peritoneal cavity. These MDSCs were highly immunosuppressive and attenuated Con A–induced hepatitis upon adoptive transfer. TCDD administration in naive mice also led to induction of several chemokines and cytokines in the peritoneal cavity and serum (CCL2, CCL3, CCL4, CCL11, CXCL1, CXCL2, CXCL5, CXCL9, G-CSF, GM-CSF, VEGF, and M-CSF) and chemokine receptors</p> ... Show More
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