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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 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
Fri Jul 05 2013
Journal Name
Pharmacie Globale International Journal Of Comprehensive Pharmacy
SYNTHESIS OF NEW PROPRANOLOL DERIVATIVES AS POSSIBLE PRODRUGS
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Propranolol is a nonselective-adrenergic blocker used in the treatment of hypertension, cardiac arrhythmias, and angina pectoris. A significant problem in propranolol therapy is that it undergoes extensive presystemic metabolism after oral administration leading to reduced bioavailability. In this study, two new propranolol derivatives have been designed, synthesized and characterized. These compounds were formed by acylation of propranolol followed by nucleophilic substitution reaction of acylated propranolol, these derivatives were analyzed for IR, CHN, melting points, and evaluated for their lipophilic properties compared with propranolol. The lower partition coefficient of these two derivatives revealed that the prodrug approach may be

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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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Publication Date
Thu Sep 08 2022
Journal Name
Al-khwarizmi Engineering Journal
Assessment of Ornamental Plants Tolerance for Acute Exposure of Acetaminophen and Methylparaben in Constructed Wetlands- a Preliminary Study
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The study aims to select suitable ornamental plant species that can survive relatively with high concentrations of acetaminophen and methylparaben in constructed wetlands. Alternanthera spp, Asparagus aethiopicus and Chlorophytum comosum are examined to withstand three initial concentrations, 20, 100 and 200 mg/L of acetaminophen and methylparaben. A total of 21 plastic pails with each 3 L capacity consisting of nine pails are used for each pharmaceutical and personal care products (PPCPs) compounds (acetaminophen and methylparaben) for three ornamental plants (Alternanthera spp, Asparagus aethiopicus and Chlorophytum comosum), with three pails as plant controls. The results reveales

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Effect of some induce chemical and biological agents against (Tilletia tritici (Bjerk) and T.laevis (Kühn) causal agents of wheat Common bunt disease
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This study was conducted to evaluate the efficiency of some chemicals and biological agents to induce systemic resistance (ISR) against to wheat common bunt disease caused by the two species of fungus Tilletia tritici (Bjerk.) Wint (T. caries (Dac.) Tul.) and T. laevis Kuhn (T. foetida (Wall.) Liro. Trails in the efforts to find an alternative, safe and environmentally friendly means to control the disease. Results of this study which carried out during two consecutive seasons for the years 2012 - 2013 and 2013 - 2014 at two different environmental locations. Seed treatment by (SA 100 and 200 mg/L, 500 ?–aminobutyric acid (BABA) and 1000 mg/L, Effective Microorganisms (EM1) 40 and 150 ml/kg seeds) have led to high significant redu

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Publication Date
Sun Dec 01 2013
Journal Name
Baghdad Science Journal
Detection of Anti-Helicopacter pylori IgG Antibody, Anti-GAD antibody, Anti-Beta islets cell in a sample of serum with type-2 Diabetes mellitus patients
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We have investigated twenty five patients with type-2 diabetes mellitus aged (35-60) years and fifteen healthy persons as control group to detect Anti-Helicobacter pylori IgG antibody. All studied groups were carried out to measure fasting blood sugar, anti- Glutamic acid decarboxylase (GAD), anti-? islets cells antibody by IFAT, Anti-H. pylori IgG antibody by ELISA technique. There was significant elevation in the concentration of fasting blood sugar than in control group (P < 0.05), the patients had negative results for anti-GAD antibody and anti- ? islets cells antibody, there were significant differences (P < 0.05) of anti-H. pylori IgG antibody in 28 % of patients had type-2 diabetes than control group. This lead to suggestion that typ

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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis of some heterocyclic derivatives of 1,8-Naphthyridine with a new substitution on the Naphthyridine ring
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Abstract The Synthesis in good yields of some new 1,8-Naphthyridine derivatives (1-9) and characterized on the basis of IR and 1H NMR spectra data. The compounds (1) and (6) were utilized as a starting material for the preparing of these compounds.

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Publication Date
Tue Aug 01 2023
Journal Name
Chemical Engineering Research And Design
Improvements in hydrogen evolution through a new design of coupling inexpensive nanocomposite electrocatalysts driven by high-voltage electrolysis
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Publication Date
Wed Sep 12 2012
Journal Name
Journal Of Engineering
Design and Implementation of a Vlsm Simulator
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Variable-Length Subnet Masks (VLSM), often referred to as "subnetting a subnet", is used to maximize addressing efficiency. The network administrator is able to use a long mask on networks with few hosts, and a short mask on subnets with many hosts. This addressing scheme allows growth and does not involve wasting addresses. VLSM gives a way of subnetting a network with minimal loses of IP addresses for a specific range. Unfortunately, the network administrator has to perform several mathematical steps (or use charts) to get the required results from VLSM. In this paper, a simple graph simulator is proposed (using Visual Basic 6.0 Language) to perform all the required mathematical steps and to display the obtained required information (the

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Publication Date
Fri Jul 21 2023
Journal Name
Journal Of Engineering
Design and Implementation of a Vlsm Simulator
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Variable-Length Subnet Masks (VLSM), often referred to as "subnetting a subnet", is used to maximize addressing efficiency. The network administrator is able to use a long mask on networks with few hosts, and a short mask on subnets with many hosts. This addressing scheme allows growth and does not involve wasting addresses. VLSM gives a way of subnetting a network with
minimal loses of IP addresses for a specific range. Unfortunately, the network administrator has to perform several mathematical steps (or use charts) to get the required results from VLSM. In this paper, a simple graph simulator is proposed (using Visual Basic 6.0 Language) to perform all the required mathematical steps and to display the obtained required informatio

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