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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 Jun 08 2020
Journal Name
Systematic Review Pharmacy
Synthesis and Biological Activity of Some New Thiazolidinone Derivatives
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The compound [G1] was prepared from the reaction of thiosemicarbazide with para-hydroxyphenylmethyl ketone in ethanol as a solvent. Then by sequence reactions prepared [G2] and [G3] compounds. The compound [G4] reaction with ethyl acetoacetoneto synthesized compound [G6] and acetyl acetone to synthesized compound [G5]. Reaction the [G3] with two different types of aldehydes in the present of pipredine to form new alkenes compounds [G7]and [G8].The compound [G3] reacted with hydrazine hydrate to formation[G4] with present the hydrazine hydrade 80% in (10) ml of absolute ethanol. Latter the compound [G4]reacted with different aldehydes with present the glacial acetic acid and the solvent was ethanol to formed the Schiff bases compounds[G9] an

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Publication Date
Thu Mar 19 2020
Journal Name
Systematic Review Pharmacy
Synthesis and Biological Activity of Some New Thiazolidinone Derivatives
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The compound [G1] was prepared from the reaction of thiosemicarbazide with para-hydroxyphenylmethyl ketone in ethanol as a solvent. Then by sequence reactions prepared [G2] and [G3] compounds. The compound [G4] reaction with ethyl acetoacetoneto synthesized compound [G6] and acetyl acetone to synthesized compound [G5]. Reaction the [G3] with two different types of aldehydes in the present of pipredine to form new alkenes compounds [G7]and [G8].The compound [G3] reacted with hydrazine hydrate to formation[G4] with present the hydrazine hydrade 80% in (10) ml of absolute ethanol. Latter the compound [G4]reacted with different aldehydes with present the glacial acetic acid and the solvent was ethanol to formed the Schiff bases compounds[G9] an

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Publication Date
Mon Feb 20 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis of Some New 2-thioxoimidazolidin-4-one Derivatives
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This research includes the synthesis of new series of heterocyclic compounds. Reaction of 2-nitro benzylidene)thiosemicarbazide(1) with ethyl chloro acetate gave (2-nitro benzylidene amino)-2-thioxomidazolidine-4-one(2) ,treatment(2) with methyl iodide to give(3)which was reacted with hydrazine to give 2-hydrazinyl-1-[(2-nitrobenzylidene)amino]- 1H-imidazol-5(4H)-one, andreation of compound(2) with aromatic aldehydes to give 5arylidene -3-({2-nitro benzylidene}amino)2-thioxo-3,5-dihydro-4H-imidazole-4-one(5a,5b), which was reacted with ethyl aceto acetate to give 4-aryl-1-[2-nitrobenzylidene, amino -6oxo-2-thioxo octa hydro-1H-benzo[d]imidazole-5-carboxylate and followed synthesis of βlactamederivtives(9a,9b) by treatment derivatives(

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Publication Date
Thu Mar 16 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis of Some New Heterocyclic Compounds Via Chalcone Derivatives
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  The chalcones 1( a,b) were prepared by the reaction of  2- acetyl benzofuran with two aromatic aldehydes in the presence of alkaline media. These chalcones are used as starting material to obtain the  desired heterocyclic: pyrazolin, isoxazoline, pyrimidinthion, pyrimidinone, cyclohexanone and indazole derivatives. The structure of newly synthesized heterocyclic compounds were established on the basis of  their melting points, elemental analysis(C.H.N), FTIR and 1HMNR (for some of them) spectral data . The synthesized compounds have been screened for their antibacterial activities, they exhibited good antibacterial activity against Escherichia coli (G-) and Staphylococus aureus (G+) . 

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis of New Some Imidazole Derivatives Containing ?-Lactam Ring
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In this work 5-methylene-yl - (2-methy –oxazole-4-one) (1H) imidazole (1) were synthesized from the reaction of L-Histidine with acetic anhydride and which converted to the of 5-methylene-yl-(2-methyl 3-amino imidazole-4-one)-1H-imidazole (2) by reaction with hydrazine hydrate. Schiff bases (3-6) were synthesized from the reaction of compound (2) with different aromatic aldehyde. Reaction of compounds (3-6) with chloroacetyl chloride gives azetidinone one derivatives (7-10). These compounds were characterized by FT-IR and some of them with 1H-NMR and 13C-NMR spectroscopy.

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Publication Date
Mon Oct 25 2021
Journal Name
Iraqi Journal Of Science
Synthesis of Some New Bis- 2, 3-Dihydroquinazolin-4(1H)-one Derivatives from Dapsone Drug and Investigating their Liquid Crystalline Properties and Antibacterial Activities
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     During this paper, new Schiff's base derivatives [F1-F5] were prepared through the reaction of dapsone drug with different substituted benzaldehyde compounds. Schiff's bases were then converted into 2,3-dihyroquinazolin-4(1H)-one derivatives [F6-F10] through the reaction with 2-amino benzoic acid in ethanol. The synthesized compounds were identified by their physical properties using UV-Vis, FT-IR and 1H-NMR analyses. The liquid crystalline properties of some prepared compounds revealed smectic and nematic phases. Using two separate bacterial species, Pseudomonas aeruginosa (Gram -ve) and Staphylococcus  aureus<

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Publication Date
Wed Jul 01 2009
Journal Name
Journal Of The Faculty Of Medicine Baghdad
Comparative study of CA19-9 levels as tumor marker in sera and tissues of patients with stomach, colon and rectum cancers
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Background: CA19-9 is among a group of mucin glycoprotein sialosyl lewis antigen (SLA) having come to be recognized as a circulating cancer associated antigen for gastrointestinal cancer. Basic research into cancer causation will be a powerful determinant of intervention in the transformation process reinforcing the need for developing effective molecular tumor biomarkers for early detection of malignant evolution in tissues of organs i.e. stomach, colon and rectum. In this study, we make a comparsion between the levels of CA19-9 in sera and tissues of patients with these diseases to see if their levels are proportional and if it is a tumor marker that affect with malignant cells in tissues of these org

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Publication Date
Tue Jun 20 2023
Journal Name
Baghdad Science Journal
Improving propagation of Echinacea purpurea and its content of some active compounds by using Tyrosine and Salicylic acid in vitro
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The seed propagation is the predominant method of Echinacea propagation, which has been criticized for its time-consuming control over the separation factor and the uncertainty of pathogen-free plants produced by this method. The technology of tissue culture has provided multiple opportunities for the production of secondary metabolites continuously without being restricted to a specific season, due to the possibility of controlling the environmental conditions and the components of the nutrient medium needed by the plant. This study was conducted to investigate the effects of salicylic acid as elicitor and tyrosine as precursor on propagation and some secondary compounds production in coneflower in vitro. The result showed the superiori

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Publication Date
Wed Aug 28 2019
Journal Name
Revista Aus
Synthesis and Identification of New Derivative of L-ascorbic Acid with Glycine and Some Metal Complexes
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The reaction of starting materials (L-asCl2):bis[O,O-2,3;O,O-5,6-(chloro(carboxylic) methylidene)]- -L-ascorbic acid] with glycine gives new product bis[O,O-2,3,O,O-5,6-(N,O-di carboxylic methylidene N-glycine)-L-ascorbic acid] (L-as-gly) which is isolated and characterized by, Mass spectrum UV-visible and Fourier transform infrared spectrophotometer (FT-IR) . The reaction of the (L-as-gly) with M+2; Co(II) Ni(II) Cu(II) and Zn(II) has been characterized by FT- IR , Uv-Visible , electrical conductivity, magnetic susceptibility methods and atomic absorption and molar ratio . The analysis showed that the ligand coordinate with metal ions through mono dentate carboxylic resulting in six-coordinated with Co(II) Ni(II) Cu(II) ions while with

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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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