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Synthesis of new Conjugates of some NSAIDs with Sulfonamide as Possible Mutual Prodrugs using Tyrosine Spacer for Colon Targeted Drug Delivery
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The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of  inflammation and infections in colon).

Key words: Mutual prodrug, Ester linkage, Azo bond, Colon targeting

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Publication Date
Mon Dec 30 2024
Journal Name
Wasit Journal For Pure Sciences
A New Class of Higher Derivatives for Harmonic Univalent Functions Established using a Generalized Fractional Integral Operator
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A new class of higher derivatives  for harmonic univalent functions defined by a generalized fractional integral operator inside an open unit disk E is the aim of this paper.

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Publication Date
Sun Jun 02 2019
Journal Name
Baghdad Science Journal
New Fluorometric Method for the Determination of Ketotifen Fumarate Using Continuous Flow Injection Analysis via ISNAG-fluorimeter
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        A newly developed analytical method was conducted for the determination of Ketotifen fumarate (KTF) in pharmaceuticals drugs via quenching of continuous fluorescence of 9(10H)-Acridone (ACD). The method was applied using flow injection system of a new homemade ISNAG fluorimeter with fluorescence measurements at ± 90◦ via 2×4 solar cell. The calibration graph was linear in the range of 1-45 mmol/L, with correlation coefficient r = 0.9762 and the limit of detection 29.785 µg/sample from the stepwise dilution for the minimum concentration in the linear dynamic ranged of the calibration graph. The method was successfully applied to the determination of Ketotifen fumarate in two different pharma

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Publication Date
Wed Jan 01 2020
Journal Name
Biochemical And Cellular Archives
New derivative of chitosan based on epichlorohydrne, synthesis, characterization, antibacterial activity and swelling study
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A novel series of chitosan derivatives were synthesized via reaction of chitosan with carbonyl compounds and grafted it’s by with different amine compounds substituted hydrogen. The produced polymers were characterized by different analyses FTIR, 1HCNMR, XRD, DSC and TGA. Solubility in water as well as many solvent was investigated, antibacterial activity of chitosan and its derivatives against two types of bacteria E. coli and S. aureus was also investigated. The results showed that derivatives sort of have antibacterial activities against Esherichia coli (Gram negative) better than chitosan whilst compound IX has better antibacterial against Staphylococcus aureus (Gram positive). SEM analysis showed that increase of surface roughness wi

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Publication Date
Sat Dec 01 2018
Journal Name
Journal Of Pharmaceutical Sciences And Research
Synthesis and biological activity of new esters derived from D-fructose-containing isoxazole moiety
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Background: Isoxazoles are an important class of five-membered unsaturated heterocyclic compounds. They show several applications in diverse areas such as pharmaceuticals, agrochemistry and industry. Isoxazoles are also found in natural sources showing insecticidal, plant growth regulation and pigment functions. Current study was conducted for synthesis of twenty five new Isoxazole derivatives and to evaluate the in vitro antibacterial activities of these derivatives. Methods: Benzaldoxime and their substituted [I] ae were prepared via addition-elimination reactions between aromatic aldehyde and hydroxylamine hydrochloride. In a second step, para-or meta-substituted benzaldoximes [I] ae were reacted with N-chlorosucceinimide in DMF to yield

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Publication Date
Thu Mar 16 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis and Characterization of New Phthalimides Containing 1, 2, 4-triazole and Imine Group
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Several new derivatives of 1, 2, 4-triazoles linked to phthalimide moiety were synthesized through following multisteps. The first step involved preparation of 2, 2-diphthalimidyl ethanoic acid [2] via reaction of two moles of phthalimide with dichloroacetic acid. Treatment of the resulted imide with ethanol in the second step afforded 2, 2-diphthalimidyl ester [3] which inturn was introduced in reaction with hydrazine hydrate in the third step, producing the corresponding hydrazide derivative [4]. The synthesized hydazide was introduced in different synthetic paths including treatment with carbon disulfide in alkaline solution then with hydrazine hydrate to afford the new 1, 2, 4-triazole [10]. Reaction of compound [10] with different alde

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Publication Date
Mon Dec 01 2014
Journal Name
Journal Of Al-nahrain University
Synthesis and Liquid Crystalline Behavior of New Amides and Esters Containing 7,1-Thiazole Ring
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Synthesis and study liquid crystalline properties of new compounds with terminal groups of amides ([III]a-c,[IV]a-c and [VI]n), alkoxy series[V]n or ester with azo linkage ([IX]a-c and[X]a-c) containing thaizole ring. These series were synthesized by many steps starting from 4- hydroxyacetophenone or 4-aminoacetophenone. The synthesized compounds were characterized using melting points, FTIR, C.H.N.S analysis and for some of them 1H NMR spectroscopy. The liquid crystalline properties were studied by hot stage polarizing microscopy and differential scanning calorimetry DSC. All compounds of series [III]a-c,[IV]a-c and compounds [V]n showed enantiotropic liquid crystal. While the series [VI]n showed nematic mesomorphism except [VI]8 did not s

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Publication Date
Tue Feb 12 2013
Journal Name
International Journal Of Engineering Sciences And Research Technology
Synthesis, Characterization of New Azo Compounds and Studies Effect on the Ach Enzyme(Invitro)
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Three azo compounds were synthesized in two different methods, and characterized by FT-IR, HNMR andVis) spectra, melting points were determined. The inhibitory effects of prepared compounds on the activity of human serum cholinesterase have been studied in vitro. Different concentrations of study the type of inhibition. The results form line weaver-Burk plot indicated that the inhibitor type was noncompetitive with a range (33.12-78.99%).

Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New Mannich Bases Derived from 7-hydroxy-4-methyl Coumarin
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Coumarin is a natural substance isolated from different plants. It belonges to a group of benzobyrones which consists of a benzene ring joined to a pyrone nucleus. In the present research, a new series of coumarin derivatives were formed. Compound (1) (7-hydroxy-4-methyl Coumarin) was converted into 4-methylquinolin-2(H) derivative (2) by reaction with acetamide, and then reaction of (2) with thiosemicarbazide in ethanol leads to the synthesize of hydrazincarbothioamide derivative (3).The reaction of (3) with ethylchloroacetate in presence of sodium acetate leads to closure ring to get [(1-(5-oxo-2-thioxoimidazolidin-1-ylimino) ethyl)]quinolin-2(1H)-one (4). Mannich bases were prepared through the reaction of (4) with primary

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Publication Date
Fri Mar 25 2016
Journal Name
Oriental Journal Of Chemistry
Synthesis and Antioxidant Ability of New 5-amino-1,2,4-Triazole Derivatives Containing 2,6-dimethoxyphenol
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4-amino-3-(4-(((4-hydroxy-3,5dimethoxybenzyl)oxy)methyl)phenyl)-1,2,4-triazole-5-thione was synthesized by to method the first one from melt reaction of 4-(((4-hydroxy-3,5-dimethoxybenzyl)oxy)methyl)benzoic acid with Thiocarbonyldihydrazide, the second method from convert the corresponded acid hydrazide to potassium 2-(4-(((4-hydroxy-3,5-dimethoxybenzyl)oxy)methyl)benzoyl)hydrazinecarbodithioate salt then react with hydrazine hydrate. Newly Schiff base (7a-7f) were synthesized from reaction the 4-amino-1,2,4-triazol with substituted hydroxybenzaldehyde. The resulting compounds were characterized by IR, 1H-NMR, 13C-NMR, and HRMS data. 2,2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) assays were used to scree

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Publication Date
Thu Jun 18 2020
Journal Name
Biochem. Cell. Arch.
NEW DERIVATIVE OF CHITOSAN BASED ON EPICHLOROHYDRNE, SYNTHESIS, CHARACTERIZATION, ANTIBACTERIAL ACTIVITY AND SWELLING STUDY
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A novel series of chitosan derivatives were synthesized via reaction of chitosan with carbonyl compounds and grafted it’s by with different amine compounds substituted hydrogen. The produced polymers were characterized by different analyses FTIR, 1HCNMR, XRD, DSC and TGA. Solubility in water as well as many solvent was investigated, antibacterial activity of chitosan and its derivatives against two types of bacteria E. coli and S. aureus was also investigated. The results showed that derivatives sort of have antibacterial activities against Esherichia coli (Gram negative) better than chitosan whilst compound IX has better antibacterial against Staphylococcus aureus (Gram positive). SEM analysis showed that increase of surface roughness wi

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