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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
Sat Dec 29 2018
Journal Name
Journal Of Global Pharma Technology
Synthesis, Characterization and Study Biological Activity of Some New Compounds Derived From Phthalic Anhydride
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In this research , phthallic anhydride ring is opened with 4-methyl aniline and acetone as a solvent to results the compound [I] that reacted with dimethyl sulphate and anhydrous sodium carbonate formation to phathalate ester [II], while the acid hydrazide compound [III], was obtained from mixed the compound [II]with hydrazine hydrate, Synthesis four type of shiff bases[IV]a-d was synthesized from the reaction of acid hydrazide [III] with aromatic aldehyde or ketone , when reacted Shiff bases with phthalic anhydride or naphthalicanhydride,I get eight derivatives of oxazepine [V]a-d , [VI]a-d. The bacterial activity of the new compounds studied by four species of bacteria: Esherichia Coli, Enterobactecloacae (Gram negative) and staphylococcu

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Publication Date
Sun Dec 20 2020
Journal Name
Journal Of Global Pharma Technology
Synthesis, Characterization, Antibacterial and Antifungal Activity of Some Bis (1, 3, 4-oxadiazole) Polymer
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Pyridine-2, 6-dicarbohydrazide comp (2) was synthesized from ethanolic solution of diethyl pyridine-2, 6- dicarboxylate comp (1) with excess of hydrazine hydrate. Newly five polymers (P1-P5) were synthesized from reaction of pyridine-2, 6-dicarbohydrazide comp (2) with five different di carboxylic acid in the presence of poly phosphoric acid (PPA). The antibacterial activity of the synthesized polymers was screened against some gram positive and gram negative bacteria. Antifungal activity of these polymers was evaluated in vitro against some yeast like fungi such as albicans (candida albicans). Polymers P3, P4 and P5 exhibited highest antibacterial and antifungal against all microorganisms under test.

Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis And Characterization Of Some New Acetylenic Mannich Bases Based On Biphenyl – 4,4 - Dithiol
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One of the most important , compound which have active hydrogen is the compound possessing (thiol group) Biphenyl-4,4-dithiol is agood example utilized in a wide field for preparation mannich bases , avariety of new acetylenic mannich bases have been Synthesized and all proposed structure were Supported by FTIR , 1H – NMR, 13C-NMR , Elemental analysis and microbial study .

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Publication Date
Sun Nov 06 2022
Journal Name
Hiv Nursing
Synthesis, Structural Characterisation and Biological Activity of New Mannich Compounds Derived from Cyclohexanone Moiety
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The formation and structural investigation of three new Mannich bases are reported. The synthesis of these compounds was accomplished via a multicomponent one-pot reaction using CaCl2 as a catalyst. The reaction of the benzaldehyde, m-bromoaniline and cyclohexanone or 4-methylcyclohexanone resulted in the formation of L1 and L3, respectively. The synthesis of L2 was achieved by mixing benzaldehyde, o-bromoaniline and cyclohexanone. The isolated compounds were characterised using a range of analytical and spectroscopic techniques. These include; NMR (1H and 13C-NMR), ESMS, FTIR, electronic spectroscopy, microanalyses and melting points. The NMR data for L1 and L2 indicated the presence of one isomer in solutions, on the NMR time scale. How

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Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Design, Synthesis, Characterization and Comparative Cytotoxic Evaluation of bis-(2- mercaptoacetate) gold (III) chloride
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In recent years , the interest in gold (III) species have gained more and more attention for cancer chemotherapy , this was stimulating by the possibility to develop new agents with mode of action and clinical profile different from the established platinum metalodrugs.

With this frame, recently new square planar Au(III)  complexes (Au(L)(L')n); where L=SCH2COO- ; L'=HSCH2COO- had been synthesized with S/O – donor ligands.

In this article and by the aim to replace, one of (L') ligand by anion chloride ligand (which supposedly more relevant for the biodistribution of the compound than for its pharmacodynamic effects), new complex (Au(L')

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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
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 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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Publication Date
Sun Jan 01 2023
Journal Name
Dental Hypotheses
Revolutionizing Systematic Reviews and Meta-analyses: The Role of Artificial Intelligence in Evidence Synthesis
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Publication Date
Thu Oct 03 2024
Journal Name
Pharmacia
Synthesis and preliminary antimicrobial evaluation of new 7-amino-4-methyl-coumarin thiazolidinone conjugates
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Abstract As a part of our ongoing project on the design and synthesis of new 4-thiazolidinone derivatives with antimicrobial activity, four new 4-thiazolidinone derivatives carrying bromo, nitro, methyl, and chloro groups on the benzene ring were synthesized by starting with the 7-amino-4-methylcoumarin moiety, linking coumarin with various phenyl isothiocynate to form the thiourea group, and then cyclizing the derivatives, characterized by IR and 1HNMR, and assayed in vitro for their antimicrobial activity against Gram positive and Gram negative bacteria and fungi. Overall, 2-(4-methyl-2-oxo-2H-chromen-3-yl)-3-(4-nitrophenyl) thiazolidin-4-one to be the most powerful individuals in the series. Based on the observed data, it can be sta

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