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Synthesis of 5-Fluorouracil Derivatives as Possible Mutual Prodrugs with Meloxicam and Ibuprofen for Targeting Cancer Tissues
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In the present study, five derivatives have been designed to be synthesized as possible mutual prodrugs for 5-Fluorouracil (5-FU) and non steroidal anti-inflammatory drugs (NSAIDs) to selectively deliver the drugs into the cancer cells. The synthesis of the target compounds were accomplished following multistep reaction procedures, the chemical reaction followed up and the purity of the products were checked by TLC. The structure of the final compounds and their intermediates were confirmed by their melting points, infrared spectroscopy and elemental microanalysis, the hydrolysis of compound III was studied using HPLC technique. According to the results mentioned above, compounds (I−V) can be good candidates as possible mutual prodrugs of 5-FU and NSAIDs that can selectively deliver the parent drugs into the cancer cells by the effect of enzymes that elevated in tumor tissues compared with normal tissues.

Key wards: Anticancer, 5-Fluorouracil, NSAIDs, prodrug.

 

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Publication Date
Wed Sep 02 2020
Journal Name
International Journal Of Drug Delivery Technology
Synthesis of Levofloxacin Derivatives with some Amines and their Complexes with Copper(II) Salts and Evaluation of their Biological Activity
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Levofloxacin belongs to the fluoroquinolone family; it is a potent broad-spectrum bactericidal agent. The pharmacophore required for significant antibacterial activity is the C-3 carboxylic acid group and the 4-pyridine ring with the C-4 carbonyl group, into which binding to the DNA bases occur. In this work, we tried to show that by masking the carboxyl group through amide formation using certain amines to form levofloxacin carboxamides, an interesting activity is kept. Levofloxacin carboxamides on the C-3 group were prepared, followed by the formation of their copper complexes. The target compounds were characterized by FT-IR, elemental analysis. The antimicrobial activity of the target compounds was evaluated and showed satisfactory resu

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis and Spectroscopic Characterization for Some Metal ion Complexes with 2-Hydroxy-3-((5-Mercapto-1,3,4-Thiadiazol-2-yl)Diazenyl)-1-Naphthaldehyde
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New metal ion complexes were synthesized with the general formula; K[PtLCl4], [ReLCl4] and K[ML(Cl)2] where M = Pd(II), Cd(II), Zn(II) and Hg(II), from the Azo ligand (HL) [2-Hydroxy-3-((5-mercapto-1,3,4-thiadiazol-2-yl)diazenyl)-1-naphth aldehyde] (HL) the ligand was synthesized from (2-hydroxy-1-naphthaldehyde) and (5-amino-1,3,4-thiadiazole-2-thiol). The ligand and its metal complexes are characterized by phisco- chemical spectroscopic techniques (FT.IR, UV-Vis and Mass spectra, elemental analysis, molar conductivity, Atomic Absorption, Chloride contain and magnetic susceptibility). The spectral data suggest that the (HL) behaves as a bidentate ligand in all complexes. These studies revealed tetrahedral geometries for all metal complexes

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Publication Date
Fri Sep 03 2021
Journal Name
Tropical Journal Of Natural Product Research
Hematological and Histopathological Changes in the Spleen of Male Albino Rats (Rattus norvegicus) Treated with Meloxicam
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Publication Date
Fri Jan 01 2016
Journal Name
Chemistry And Materials Research
Synthesis of Triazolo and Pyrazolo Derivatives of Quinoline Nucleus
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New heterocyclic derivatives of quinoline are reported. Reaction of quinoline-2-thiol 4 with hydrazine hydrate gave 2-hydrazionoquinoline 5. Treatment of 5 with CS2 in pyridine afforded 1,2,4-triazolo-[4,3-a]- quinolin-1-2H-thione 6, whereas the reaction of 5 with carboxylic acids namely formic acid or acetic acid, yielded the 1,2,4-triazol-[4,3-a]-quinolin 7 or 5-methyl-1,2,4-triazolo [4,3-a]-quinoline 8 through ring closure. Diazotization of 5 under acidic conditions produced the fused tetrazole compound 9, tetrzolo-[1,5-a]- quinoline. Moreover, treatment of 5 with active methlyene compounds gave two pyrazole derivatives 10 and 11. Azomethines 12a-e were prepared through condensation of 5 with aromatic aldehydes or ketones.

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Publication Date
Tue Apr 30 2024
Journal Name
Iraqi Journal Of Science
Synthesis and Characterization of some new heterocyclic derivatives from aromatic carbonyl ‎compounds and carboxylic acids with Evaluation some of them for biological activity
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     In this research investigation, a total of eighteen diverse tetra- and penta-lateral cyclic compounds were synthesized. These included 1,3,4-thiadiazole, thiazolidin-4-one (via an alternative method), 1,2,4-triazole, carbothioamide, thiazole-4-one, azetidin-2-one, and oxazole. The synthesis procedure entailed a sequence of reactions. The thiazolidine-4-one 1 was obtained by reaction p-aminobenzoic acid with thiosemicarbazide, followed by treatment with p-tolualdehyde to produce Schiff base 2. Reaction Schiff base 2 with mercaptoacetic acid in dry benzene was carried out to produce thiazolidine-4-one 3. In another synthesis pathway, the esterification of p-nitro benzoic acid with ethanol in the presence of sulfuric acid was

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Publication Date
Sun Jun 02 2013
Journal Name
Baghdad Science Journal
Synthesis of New Pyrazoline - Phenoxathiin Derivatives
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Phenoxathiin was prepared by the reaction of diphenyl ether with sulfur in the presence of anhydrous aluminum chloride. This work comprised the synthesis of new phenoxathiin derivatives containing heterocyclic moieties. These heterocyclic compounds were synthesized in three groups. The first group was made up of 2-(oxoalken-1-yl) phenoxathiin derivatives (3a-3j) obtained from the reaction of 2-acetylphenoxathiin with different aromatic aldehyde in the presence of sodium hydroxide. The other two groups involved compounds produced from the reaction of (3a-3j) with hydrazine hydrate in acetic acid to get 2-(1-acetyl pyrazolin-3-yl) phenoxathiin derivatives (4a-4j), and phenyl hydrazine in the presence of piperidine to afford 2-(1-phenyl pyrazo

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Publication Date
Wed Jan 14 2009
Journal Name
Diala , Jour
Synthesis of Barbiturate Derivatives from Imines
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Publication Date
Mon Jun 25 2018
Journal Name
International Journal Of Pharmaceutical Quality Assurance
Synthesize of New Ibuprofen and Naproxen Sulphonamide Conjugate with Anti-Inflammatory Study and Molecular Docking Study
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Non-steroidal anti-inflammatory drugs (NSAIDs) contain free –COOH which thought to be responsible for the GI irritation associated with all traditional NSAIDs. The esterification of this group is one of an approach to ultimate aim for reduce the gastric irritation; so in this study we synthesized and preliminarily evaluated new ester compounds as new analogues with expected selectivity toward COX-2 enzyme. Synthetic procedures have been successfully developed for the generation of the target compounds (III a and b). The synthetic approach involved multi-steps procedures which include: Synthesis of 4-hydroxy benzene sulphonamide ( I b ), synthesis of Naproxen and Ibuprofen acyl chloride and then reacting them with 4-hydroxy benzene sulphon

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Publication Date
Wed May 22 2024
Journal Name
Al-rafidain Journal Of Medical Sciences ( Issn 2789-3219 )
Assessment of Urine and Serum Exosomes as Biomarkers for the Diagnosis of Bladder Cancer
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Background: Bladder cancer (BC) is the most common malignant tumor in the urinary tract and the tenth most common malignancy worldwide. Exosomes are 40–100 nm-diameter nanovesicles that are either released straight from the plasma membrane during budding or merged with the plasma membrane by multivesicular bodies. Objectives: To assess the proportion of serum and urinary Exosome levels in urinary bladder cancer patients, as well as their impact on the disease. Methods: From January 2023 to June 2023, a total of 45 samples of blood and urine were collected from individuals diagnosed with bladder cancer at the Ghazi Hariri Hospital for Specialized Surgery. They included 45 male and female patients, varying in age, as well as 45 heal

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Publication Date
Thu Jan 11 2024
Journal Name
Tropical Journal Of Pharmaceutical Research
Application of Taguchi orthogonal array in optimization of the synthesis and crystallinity of metal organic framework 5 (MOF 5)
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Purpose: To use the L25 Taguchi orthogonal array for optimizing the three main solvothermal parameters that affect the synthesis of metal-organic frameworks-5 (MOF-5). Methods: The L25 Taguchi methodology was used to study various parameters that affect the degree of crystallinity (DOC) of MOF-5. The parameters comprised temperature of synthesis, duration of synthesis, and ratio of the solvent, N,N-dimethyl formamide (DMF) to reactants. For each parameter, the volume of DMF was varied while keeping the weight of reactants constant. The weights of 1,4-benzodicarboxylate (BDC) and Zn(NO3)2.6H2O used were 0.390 g and 2.166 g, respectively. For each parameter investigated, five different levels were used. The MOF-5 samples were synthesi

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