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Synthesis and Preliminary Pharmacological Evaluation of New Analogues of Diclofenac as Potential Anti-inflammatory Agents

         A group of amine derivatives [4-aminobenzenesulfonamide derivatives, 2-aminopyridine and 2-aminothiazole] incorporated to α-carbon of diclofenac a well known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were designed and synthesized for evaluation as  a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of the selected final compounds (9, 12 and 13) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (3 mg/Kg) of diclofenac sodium. All tested compounds  produced a significant reduction  in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the 4-aminobenzenesulfonamide derivative (compound 9) exhibited superior anti-inflammatory activity compared to diclofenac sodium at times 180-300 minutes with the same onset of action. The results of this study indicate that the incorporation of the selected aromatic amino groups in to diclofenac maintain its anti-inflammatory activity.                                                                                                                             

Key words: amine derivatives, anti-inflammatory, diclofenac derivatives, COX-2 selectivity.                                                                                                 

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Publication Date
Fri Mar 07 2025
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of frictional forces generated by different brackets and orthodontic wires

Background: Sliding mechanics is widely used during orthodontic treatment. One of the disadvantages of this mechanics is the friction generated at the bracket/archwire interface, which may reduce the amount of desired orthodontic movement obtained. The aim of the present in vitro study was to evaluate and compare the static frictional forces produced by two passive self-ligating brackets stainless-steel and hybrid and two conventional brackets stainless-steel and monocrystal ligated with stainless-steel ligature wire at two degrees of torque(zero and twenty) under dry condition. Materials and method: One hundred and sixty brackets were used in this study divided into four groups each group consisted of forty brackets these are: Two self-li

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Publication Date
Sat Jun 03 2023
Journal Name
Iraqi Journal Of Science
Facies and Reservoir Evaluation of Mishrif Formation in Tuba Oil Field

The Mishrif Formation is one of the most important formation in oil fields, which is located in southern part of Iraq, and it is of Upper Cretaceous age. Tuba field is located nearly 40 km SW – Basrah city. It is bounded from east by Zubair oil field (5 km distance) and from west by Rumaila (2 km distance). The Tuba oil field is situated between Zubair oil field in the east and Rumaila in the west, and is separated by two depressions.
The rock (core and chips) samples have been collected systematically from cores of Mishrif Formation that are available from stores of southern oil company to prepare thin sections and slides—these slides have been examined by using microscope. These samples have been taken from all parts of the rese

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Publication Date
Sat Jul 08 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation Characterization and Evaluation of Meloxicam Nanoemulgel to be Used Topically

Meloxicam is a non-steroidal anti-inflammatory drug. It is practically insoluble in water. It is associated with gastrointestinal side effects at high doses on long  term treatment. The aim of this investigation to formulate and evaluate gellified nanoemulsion of meloxicam as a topical dosage form to enhance meloxicam therapeutic activity and reduce systemic side effect.

The pseudo ternary phase diagrams were made, including  the oil mixture which is composed of almond oil and peppermint oil at a ratio (1:2), variable surfactant mixture (S mix) which are tween 80 and ethanol at ratios of (1:1, 2:1, 3:1, and 4:1) and double distilled water. Slow dripping of double distilled water to the combination  of the oil mixtu

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Publication Date
Tue Jul 02 2024
Journal Name
Al-rafidain Journal Of Medical Sciences ( Issn 2789-3219 )
Formulation and Evaluation of Bilastine Thermosensitive Mucoadhesive Ophthalmic in situ Gel

Background: Bilastine is a non-sedating, second-generation antihistamine used to treat urticaria and allergic conjunctivitis. Objective: to formulate and test bilastine as a mucoadhesive ophthalmic in situ gel in order to extend its presence at site for longer time and help treat conjunctivitis and allergic rhinitis. Methods: We prepared formulations using different concentrations of poloxamers (Poloxamer 407 (P407) and Poloxamer 188 (P188)) in combination with hydroxypropyl methyl cellulose (HPMC). The prepared formulas were evaluated for their physicochemical properties, sol-gel transition temperature, viscosity, mucoadhesive strength, drug release, and kinetic modeling. Results: The prepared in situ gels were clear and transparen

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Publication Date
Mon Jan 01 2024
Journal Name
Journal Of Research In Pharmacy
Preparation, Evaluation, and Histopathological Studies of Ondansetron-Loaded Invasomes Transdermal Gel

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Publication Date
Thu Aug 01 2024
Journal Name
Journal Of Research In Pharmacy
Preparation and evaluation of transdermal gel loaded with spanlastics containing meloxicam

A transdermal drug delivery system (TDDS) is characterized by the application of medications onto the skin's surface to deliver drugs at a controlled and predefined rate through the skin. Spanlastics, an elastic nanovesicle capable of transporting various pharmacological substances, shows promise as a drug delivery carrier. It offers numerous advantages over traditional vesicular systems applied topically, including enhanced stability, flexibility in penetration, and improved targeting capabilities. This study aims to develop meloxicam (MX)-loaded spanlastics gel as skin delivery carriers and to look into the effects of formulation factors like Tween80, Brij 35, and carbopol concentration on the properties of spanlastics gel, like pH, drug

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Publication Date
Sun Dec 01 2019
Journal Name
Journal Of Economics And Administrative Sciences
Evaluation of waste sorting and recycling laboratory in Mahmudiya (case study)

The daily practices of humans produce various types of waste, which are a threat to the health and environment surrounding it, especially after the increase in quantities as a result of population growth and technological development, and here came the need for recycling solid waste as one of the modern concepts that achieve environmental benefits, The aim of the research is to evaluate the project of sorting and recycling of solid waste in the district of Mahmoudiya and whether its work is sustainable ,Conforming to modern standards, using standard checklists to determine the gap between the current laboratory reality and the requirements of those standards , Using the case study methodology as the most appropriate approach

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Publication Date
Sun May 14 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
A New Design of Fractal Optical Modulation

In this paper it was designed a new fractal optical modulation by using a new iteration of fractal function, the result was analyzed by MTF evaluation, and it compared with results of normal optical modulation.

The normal and fractal optical modulator is a circular disc which has a radius R=9cm, both of them consist of twenty sectors, ten sectors are opaque and the other ten sectors are transmitted for the light.

      The fractal optical modulator contains two patterns, the pattern two can be used to detect the target, and pattern one can be used to lock the target

The best similarity of MTF behavior for normal and fractal Reticle was evaluating the power transparent depends on the size o

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Publication Date
Tue Aug 03 2021
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
New Travelling Wave Solution of Burgers Equations

     In this paper, we studied the travelling wave solving for some models of Burger's equations. We used sine-cosine method to solution nonlinear equation and we used direct solution after getting travelling wave equation.

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Publication Date
Sun Mar 07 2010
Journal Name
Baghdad Science Journal
Antifungal Activity of Some New Binuclear Complexes

Three complexes of copper(II) and iron(II) with mixed ligands acetylacetonebis(thio-semicarbazone)- ABTSH2 and benzaldazine- BA have been prepared and characterized using different physico-chemical techniques including the determination of metal contents, mole-cular weight, measurement of molar conductivity, magnetic moment, molar refraction, infrared and electronic spectra. Accordingly, octahedral complexes having general formulaes [Cu2(ABTSH2)2(BA)2Cl2]Cl2 and [M2(ABTSH2)2(BA)2(SO4)2] {M= Cu(II) or (Fe(II)} have been proposed. The resulted complexes screened for antifungal activity in vitro against the citrus pathogen Aspergillus niger and Fusarium sp. which caused root rot of sugar and the beans pathogen Alternaria sp. All the complex

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