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Design, Synthesis and Preliminary Pharmacological Evaluation of New Non-Steroidal Anti-Inflammatory Agents Having a 4-(Methylsulfonyl) Aniline Pharmacophore
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A series of 4-(methylsulfonyl)aniline derivatives were synthesized in order to obtain new compounds as a potential anti-inflammatory agents with expected selectivity against COX-2 enzyme. In vivo acute anti-inflammatory activity of the final compounds 11–14 was evaluated in rat using an egg-white induced edema model of inflammation in a dose equivalent to 3 mg/Kg of diclofenac sodium. All tested compounds produced significant reduction of paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the activity of compounds 11 and 14 was significantly higher than that of diclofenac sodium (at 3 mg/Kg) in the 120–300 minute time interval, while compound 12 expressed a comparable effect to that of diclofenac sodium in the 60–240 minute time interval time, and compound 13 showed a comparable effect to that of diclofenac sodium at all experimental times. The result of this study indicates that the incorporation of the 4-(methylsulfonyl)aniline pharamacophore into naproxen, indomethacine, diclofenac and mefanamic acid maintained their anti-inflammatory activity and may increase selectivity towards the COX-2 enzyme which will be confirmed in the future by assessing COX-2: COX-1 inhibitory ratios using a whole blood assay.

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Publication Date
Thu Apr 20 2023
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Design of New V Shaped Thermotropic Liquid Crystals containing Heterocyclic
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    The characterization and design of this study of new liquid crystals with a V shape compounds containing thiazolidine-2,4-dione and 1,3-phenylene as a core unite with mesophase properties were reported. Preparation  and characterization of chloroacetic acid, water, and thiourea to produce thiazolidine-2,4-dione [I] in the presence of strong hydrochloric acid. The 4-hydreoxybenzaldehyde and n-alkyl bromide were reacted with potassium hydroxide to create the n-alkoxy benzaldehyde., then the compound [I] reacted with [II]n in presence of piperidine to produce compounds [III]n. Also, converted resorcinol to a corresponding  compound [IV] by refl

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Publication Date
Tue Nov 01 2022
Journal Name
Optik
Design new D-π-A materials for sensitizers for dye-sensitized solar cells: Quantum chemical study
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Within this paper, we developed a new series of organic chromophores based on triphenyleamine (TPA) (AL1, AL-2, AL-11 and AL-22) by engineering the structure of the electron donor (D) unit via replacing a phenyle ring or inserting thiophene as a π-linkage. For the sake of scrutinizing the impact of the TPA donating ability and the spacer upon the photovoltaic, absorptional, energetic, and geometrical characteristic of these sensitizers, density functional theory (DFT) and time-dependent DFT (TD-DFT) have been utilized. According to structural characteristics, incorporating the acceptor, π-bridge and TPA does not result in a perfect coplanar conformation in AL-22. We computed EHOMO, ELUMO and bandgap (Eg) energies by performing frequency a

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Publication Date
Sun Mar 10 2013
Journal Name
Journal Of Life Sciences And Technologies
Synthesis, Characterization, and Anti-Microbial Study of Metal Complexes of Polycyclicacetal derived from PVA & Erythro-Ascorbic acid derivative
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The aim of this work is the synthesis of new grafted PVA polymer with a derivative of Erythro-ascorbic acid (pentulosono-ɣ -lactone-2, 3-enedianisoate). All synthesized compounds were characterized by thin layer chromatography (TLC) and FTIR spectra and aldehyde was also characterized by (U.V-Vis), 1HNMR, 13CNMR and mass spectra. They were also evaluated for antimicrobial properties by dilute method against four pathogenic bacteria (Escherichia coli ,Klebsiella pneumonae, Staphylococcus aureus, Staphylococcus Albus) and two fungal (Aspergillus Niger, Yeast). All polymer metal complexes showed good activities against the various microbial isolates. The polymer metal complexes showed higher activity than the free polymer. The order of increa

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Publication Date
Tue Oct 22 2019
Journal Name
Scientia Pharmaceutica
Design, Synthesis, and Docking Study of Acyl Thiourea Derivatives as Possible Histone Deacetylase Inhibitors with a Novel Zinc Binding Group
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Histone deacetylase inhibitors with zinc binding groups often exhibit drawbacks like non-selectivity or toxic effects. Thus, there are continuous efforts to modify the currently available inhibitors or to discover new derivatives to overcome these problems. One approach is to synthesize new compounds with novel zinc binding groups. The present study describes the utilization of acyl thiourea functionality, known to possess the ability to complex with metals, to be a novel zinc binding group incorporated into the designed histone deacetylase inhibitors. N-adipoyl monoanilide thiourea (4) and N-pimeloyl monoanilide thiourea (5) have been synthesized and characterized successfully. They showed inhibition of growth of human colon adenoc

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Publication Date
Mon Dec 30 2013
Journal Name
Journal Of The College Of Basic Education
Synthesis and Antimicrobial Activities of (Mn, Co, Ni, Cu, Hg and Ag) Complexes with Poly (Vinyl-4-Aminobenzoate)
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The aim of this work is synthesis of _Eoly (Vinyl-4-AminoBenzoate) (PVAB) from reaction of _Eoly Vinyl Alkohol PVA with 4-aminobenzoyl chloride in alkaline media. We also prepare the metal complexes of poly (vinyl- 4-aminobenzoate) and antimicrobial properties were evaluated by dilute method against five pathogenic bacteria (Escherichia coli, Shigella dysentery, Klebsiella pneumonae, Staphylococcus aureus, Staphylococcus Albus) and two fungal (Aspergillus Niger, Yeast). All polymer metal complexes showed different activities against the various microbial isolates. The polymer metal complexes showed higher activity than the free polymer.

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Publication Date
Fri Dec 29 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis and Characterization of 1, 3-Oxazepine and Benz [1, 2-e][1, 3] Oxazepine-4, 7-Diones
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N-Benzylidene m-nitrobenzeneamines (Schiff bases) were prepared by condensation of m-nitroaniline with aromatic aldehydes. These Schiff bases were found to react with maleic anhydride to give 2-Aryl-3-(m-nitrophenyl)-2, 3-dihydro [1, 3] oxazepine–4, 7–diones and with phthalic anhydride to give 2-Aryl-3–(m-nitrophenyl)–2, 3–dihydrobenz|| 1, 2-e|||| 1, 3] oxazepine–4, 7-diones which were reacted with pyrrolidine to give the anilide–pyrrolidides of maleic acid and phthalic acid.

Publication Date
Thu Dec 30 2021
Journal Name
Iraqi Journal Of Science
Some Clinical and Inflammatory Aspects of Trichomonas vaginalis Infection among Women with Pelvic Inflammatory Diseases
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   Infection with Trichomonas vaginalis and its relation to some diseases have lately had much attention.  The objective of this study was to assess the infection rate of T. vaginalis and its relation to pelvic inflammatory diseases, infertility, and vaginosis. The study also assessed some demographic, clinical, and immunological parameters in women infected with T. vaginalis. The study included 160 non-pregnant married women who attended some private clinics and public hospitals in Baghdad from October 2020 to February 2021. All participants had symptoms of vaginal discharge only or vaginal discharge with lower abdominal pain. The participants were divided into an infertility group (n = 61) and fertility group (n = 99). The participant

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Publication Date
Tue Mar 01 2022
Journal Name
Iranian Journal Of War And Public Health
Histological Evaluation of Vitronectin Protein/AngiopoietinLike 4 Protein on Bone Healing in Rats
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2929-2933

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Publication Date
Thu Apr 13 2023
Journal Name
Corrosion And Protection
NEW THERMOTROPIC SYMMETRICAL MESOGENS CONTAINING HETERO RINGS: SYNTHESIS AND CHARACTERIZATION
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A variety of liquid crystals comprising heterocyclics 1,3,4-oxadiazol ring [III], aminooxazol [IV]a, and aminothiazol [IV]b were synthesized through a number of steps, beginning of the reaction of 3, 3'- dimethyl - [1, 1'-biphenyl] -4, 4'- diamin, ethyl monochloroacetate and sodium acetate to synthesize diacetate compound[I]. The diester reacted with hydrazine hydrate(N2H4-H2O) to give dihydrazide compound [II], then reacted with Pyruvic acid and phosphorous oxychloride to produce diketone compound [III]. The last compound was reacted with urea and thiourea to give aminooxazol and aminothiazol respectively. The synthesized compounds actually characterized and determined the structures by melting points, FT-IR and 1H-NMR spectroscopies. By u

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Publication Date
Sun Mar 04 2012
Journal Name
Baghdad Science Journal
Synthesis of New Mannich Bases from Indole Derivatives
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This work includes two steps of synthesis, the first one is the synthesis of indole which was prepared according to literature of the reaction of phenyl hydrazine with acetaldehyde in glacial acetic acid afforded phenyl hydrazone of acetaldehyde , this product was fused with zinc chloride to give the indole.Reaction of cyclohexanone with phenyl hydrazine using the same procedure for the preparing giving 1,2,3,4-Tetrahydrocarbazole.Second step involved synthesis of a series of (17) of mannich bases derivatives of indole and 1,2,3,4-Tetrahydrocarbazle. Mannich reaction involves the condensation of aldehyde usually formaldehyde with different secondary amine and with compound containing an activated hydrogen.The reaction illustrated by the fo

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