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bijps-413
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
Thu Feb 01 2024
Journal Name
Baghdad Science Journal
A New Green Approach of CFIA Technique for Direct Assay with a High Throughput of Sulfamethoxazole Drugs Using Condensation Reaction with NQS Agent
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A new design of manifold flow injection (FI) coupling with a merging zone technique was studied for sulfamethoxazole determination spectrophotometrically. The semiautomated FI method has many advantages such as being fast, simple, highly accurate, economical with high throughput . The suggested method based on the production of the orange- colored compound of SMZ with (NQS)1,2-Naphthoquinone-4-Sulphonic acid Sodium salt in alkaline media NaOH at λmax 496nm.The linearity range of sulfamethoxazole was  3-100  μg. mL-1, with (LOD) was 0.593 μg. mL-1 and the RSD% is about 1.25 and the recovery is 100.73%. All various physical and chemical parameters that have an effect on the stability and development of

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Publication Date
Tue Apr 24 2018
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Antifungal Activity Against of Candida Species for Some New Heterocyclic Compounds Containing Schiff Base , Oxazepine , Indoline or Imidazolo Units and Their Spectral Characterization
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       The objective of this study is to test In Vitro the twenty chemical compounds that contains Schiff base or oxazepine, indoline, imidazolo units in concentrations( 50, 100, 150) mg / dl as antifungal activity, against three pathogenic Candida species  that occur in humans. We tested one isolates of

   ) Candida albicans ,Candida glabrata and Candida krusei). All these species affect human health . The study was carried out in the Laboratory of Public Health , directly of health for the period from May 2016 to April 2017  , Candida spp isolates used in this study were collected from patients admitted at  some private c

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Publication Date
Sun Jun 03 2012
Journal Name
Baghdad Science Journal
Batch and Flow-Injection Spectrophotometric Determination of Thymol Using Procaine Hydrochloride as a New Chromogenic Reagent
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New, simple and sensitive batch and Flow-injecton spectrophotometric methods for the determination of Thymol in pure form and in mouth wash preparations have been proposed in this study. These methods were based on a diazotization and coupling reaction between Thymol and diazotized procaine HCl in alkaline medium to form an intense orange-red water-soluble dye that is stable and has a maximum absorption at 474 nm. A graphs of absorbance versus concentration show that Beer’s law is obeyed over the concentration range of 0.4-4.8 and 4-80 µg.ml-1 of Thymol, with detection limits of 0.072 and 1.807 µg.ml-1 of Thymol for batch and FIA methods respectively. The FIA procedure sample throughput was 80 h-1. All different chemical and physical e

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Publication Date
Sun Aug 13 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of New Metal Complexes of -Aminonitriles Derived from P- Methoxybenzaldehyde with Aromatic Amines
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New metal complexes of some transition metal ions [Fe(III) , Co(II) , Ni(II) and Cu(II)] of two previously prepared ligands HLI=(P-methyl anilino)- P-methoxy phenyl acetonitrile and HLII =(P-methoxy anilino)-P- methoxy phenyl acetonitrile were synthesized. The two ligands were prepared by Strecker's procedure which included the reaction of Pmethoxybenzaldehyde with p-toluidine and P-anisidine respectively. The structures of the new metal complexes were characterized by atomic absorption , i.r and U.V.-visible spectra . Magnetic susceptibilities and conductivity measurements in DMF of metal complexes were also studied. These ligands coordinate as abidentate molecules through nitrogen atoms of amino group and nitrile group except the

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Publication Date
Mon Nov 29 2021
Journal Name
Iraqi Journal Of Science
Synthesis and Polymerization of Several New Maleimides Linked to Schiff Bases and Their Copolymers with Acrylonitrile
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A series of new maleimide monomers substituted with Schiff base moieties were synthesized via acid-catalyzed condensation of 3-(N-maleimidyl)phenyl hydrazide with aromatic aldehydes and ketones. The newly synthesized monomers were introduced in free radical chain growth homopolymerization producing five new polymaleimides with pendent Schiff base moieties .The new monomers were introduced also in free radical chain growth copolymerization with acrylonitrile producing new five copolymaleimides containing pendent Schiff base moieties. The new homopolymers and copolymers are of great importance since incorporation of bulky Schiff base moieties in their repeating units exhibit them better solubility and processing properties which made them

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Publication Date
Wed Jul 07 2010
Journal Name
Al-mustansiriya J. Sci
Synthesis and Spectroscopic Studies of New Heterocyclic Azo Dye and Their Complexes with Selected Metal Ion
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Coupling reaction of 4-aminoantipyrene with 8-hydroxyqunoline gave the new bidentate azo ligand 5-(4-antipyrene azo)-8-hydroxyqunoline. Treatment of this ligand with the following metals ions (MnII, CoII, NiII, CuII and ZnII) in aqueous ethanol with a 1:2 M:L ratio yielded a series of neutral complexes of the general formula [M(L)2Cl2]. The prepared complexes were characterized using flame atomic absorption, FT.IR, UV-Vis spectroscopic as well as magnetic susceptibility and conductivity measurements. Chloride ion content were also evaluated by (Mohr Method). From above data, the proposed molecular structure for these complexes as octahedral geometry.

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
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
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
Sun Dec 04 2016
Journal Name
Baghdad Science Journal
Synthesis of new Polyimides Derived from 4- minoantipyrine
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In the present study, new five polymers of acryloyl chloride have been synthesized by reaction 4-aminoantipyrine with many substituted acid chloride (A-E). Then condensation of polyacryloyl chloride with the product in one step (A-E), in a suitable solvent in the presence amount of (Et3N) to obtain new polyimides(A1-E5). The prepared compounds were characterized by UV. FT-IR, 1H-NMR and 13C-NMR spectroscopy and measuring of other physical properties such as softening point, melting point and solublities.

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