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bijps-353
Design, Synthesis and Kinetic Study of Coumarin-Based Mutual Prodrug of 5-Fluorouracil and Dichloroacetic acid
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On the basis of known coumarin-based prodrug system, a novel coumarin-based mutual prodrug of 5-fluorouracil and dichloroacetic acid was designed, synthesized and evaluated as a promising oral chemotherapeutic agent basing on in vitro stability study in HCl buffer (pH 1.2) and in phosphate buffer (pH 7.4), as well as in vitro release study in human serum. The chemical structure of prodrug was confirmed by analyzing its FTIR, 1H NMR, 13C NMR and MS-ESI spectra. The results of in vitro kinetic study indicated that the prodrug was significantly stable in HCl and in phosphate buffers, and was hydrolyzed in human serum followed pseudo first order kinetics.

Keywords: Coumarin-based prodrug, 5-fluorouracil, Dichloroacetate, kinetics.

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Publication Date
Sat Jun 19 2021
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Antibacterial Evaluation of Some Coumarin Derivatives
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Coumarin derivatives have shown different biological activities, such as antifungal, antibacterial   antiinflammatory, and antioxidant activities, besides antibiotic resistance modulating effects, and anti-HIV, hepatoprotective, and antitumor effect. So, new coumarin derivatives (hydrazones and an amide) were synthesized through multisteps reactions. All the synthesized target compounds were characterized by FT-IR spectroscopy, 1HNMR analysis. The compounds then evaluated for their anti-bacterial activity by means of well-diffusion method against two gram-positive bacteria (Staphylococcus aureus, Streptococcus pneumoniae) and two gram-negative bacteria  (E.coli and Pseudomonas aeruginosa). The highest activity was demonstr

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Publication Date
Sun Jun 30 2013
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Kinetic Study and Simulation of Oleic Acid Esterification in Different Type of Reactors
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Esterification reaction is most important reaction in biodiesel production. In this study, oleic acid was used as a suggested feedstock to study and simulate production of biodiesel. Batch esterification of oleic acid was carried out at operating conditions; temperature from 40 to 70 °C, ethanol to oleic acid molar ratio from 1/1 to 6/1, H2SO4 as the catalyst 1 and 5% wt of oleic acid, reaction time up to 180 min. The optimum conditions for the esterification reaction were molar ratio of ethanol/oleic acid 6/1, 5%wt H2SO4 relative to oleic acid, 70 °C, 90 min and conversion of oleic 0.92. The activation energy for the suggested model was 26625 J/mole for forward reaction and 42189 J/mole for equilibrium constant. The obtained results s

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Publication Date
Tue Oct 27 2015
Journal Name
International Journal Of Pharmacy And Pharmaceutical Sciences
EVALUATION OF CHEMOPREVENTIVE RESPONSE OF PENTOXIPHYLLINE AND SILDENAFIL INCOLORECTAL CARCINOMA EXPERIMENTALLY INDUCEDIN RATS: COMPARATIVE STUDYWITH 5-FLUOROURACIL
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Objective: This study was designed to investigate some possible therapeutic mechanisms of pentoxifylline and sildenafil in the treatment of colorectal carcinoma induced by 1, 2 dimethylhydrazines in rats. Methods: Rats were allocated into seven groups, negative control, colon cancer induced by 1,2,dimethylhydrazine, 5-fluorouracil (5-FU) (50 mg/kg)-treated, pentoxifylline (PTX) (50 mg/kg)-treated, sildenafil (0.7 mg/kg)-treated groups; the two other groups set as colon cancer induced group treated with PTX (50 mg/kg) plus 5-FU(50 mg/kg) and sildenafil (0.7 mg/kg) plus 5-FU (50 mg/kg), respectively. Results: Biochemical results revealed significant elevation of serum carcinoembryonic antigen (CEA) levels, carbohydrate19-9 antigen (CA19-9) as

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Publication Date
Mon Dec 30 2013
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Kinetic Study and Simulation of Oleic Acid Esterification over Prepared NaY Zeolite Catalyst
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Esterification considers the most important reaction in biodiesel production. In this study, oleic acid was used as a suggested feedstock in order to study and simulate production of biodiesel. The batch esterification reaction of oleic acid was carried out at various operating conditions; temperature from 40 to 70 °C, ethanol to oleic acid molar ratio from 3/1 and 6/1 and a reaction time up to 180 min.
The catalyst used was prepared NaY zeolite, which is added to the reaction mixture as 2, 5 and 10 wt.% of oleic acid.
The results show that the optimum conditions, gives 0.81 conversion of oleic acid, were 6/1 molar ratio of ethanol/oleic acid, 5 wt.% NaY relative to initial oleic acid, 70°C and 60 minutes. The activation energy o

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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)
Synthesis and Antimicrobial Study of Possible Mutual Prodrugs of Amoxicillin and Metronidazole by Direct and Indirect Coupling through Spacer
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Amoxicillin have been conjugated with metronidazole as possible mutual prodrug to get a wider spectrum of activity by acting on aerobic and anaerobic bacteria, have antifungal activity, to provide protection for beta lactam ring of amoxicillin and also to improve patient compliance as it given as a single dose therapy. The structures of the synthesized compound were confirmed and characterized using elemental microanalysis (CHN), IR and some physiochemical properties. Biological study was done by using  disc diffusion method against different bacterial strains which are , Staphylococcus aureus , Salmonella typhie , Pseudomonas aeruginosa , E. coli , Klebsiella pneumonia and fungi ( Candida albicans) . using nutrien

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Publication Date
Fri Apr 01 2005
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis and Characterization of Schiff Base Folic Acid Based Ligand and Its Complexes
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D-mannose sugar was used to prepare [benzoic acid 6-formyl-2,2-dimethyl-tetrahydrofuro[3,4-d][1,3]dioxol-4-yl ester] (compound A). The condensation reaction of folic acid with (compound A) resulted in the formation of new ligand [L]. These compounds were characterized by elemental analysis CHN, atomic absorption A.A, (FT-I.R.), (U.V.-Vis), TLC, E.S. mass (for electrospray), molar conductance, and melting point. The new tetradentate ligand [L], reacted with two moles of some selected metal ions and two moles of (2-aminophenol), (metal : ligand : 2-aminophenol) at reflux in water medium to give a series of new complexes of the general formula K2[M2(L)(HA)2] where M= Co(II), Ni(II), Cu(II) and Cd(II). These complexes were characterized by elem

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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 Schiff Base Folic Acid Based Ligand and Its Complexes
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D-mannose sugar was used to prepare [benzoic acid 6-formyl-2, 2-dimethyl-tetrahydrofuro [3, 4-d][1, 3] dioxol-4-yl ester](compound A). The condensation reaction of folic acid with (compound A) resulted in the formation of new ligand [L]. These compounds were characterized by elemental analysis CHN, atomic absorption AA,(FT-IR),(UV-Vis), TLC, ES mass (for electrospray), molar conductance, and melting point. The new tetradentate ligand [L], reacted with two moles of some selected metal ions and two moles of (2-aminophenol),(metal: ligand: 2-aminophenol) at reflux in water medium to give a series of new complexes of the general formula K2 [M2 (L)(HA) 2] where M= Co (II), Ni (II), Cu (II) and Cd (II). These complexes were characterized by eleme

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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)
Synthesis and Antimicrobial Evaluation of New 6 and7 Substituted Derivatives of Coumarin
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A series of benzohydrazide derivatives attached to coumarin moiety at position 6 and 7 have been synthesized. The reaction of coumarin derivatives (coumarin I and II) with p-nitrophenyl hydrazine yield Schiff bases (compound1a and IIa).These Schiff bases were refluxed with benzoyl chloride to give benzohydrazide derivatives of coumarin substituted at its 6 or 7 nucleus position (Ia1 and IIa1).The reaction and the purity of the products were checked by thin layer chromatography (TLC). The structures of the final compounds  and  their intermediates were confirmed by their melting points, infra red spectroscopy, and elemental microanalysis(CHN).

Compounds (Ia1 and IIa1) were evaluated for&n

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of New Coumarin and 2-quinolone Derivatives with Expected Biological Activities
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A series of new coumarin and N-amino-2-quinolone derivatives have been synthesized. The reaction of coumarin (1) with excess of  Hydrazine hydrate 98% yielded 1-amino-2-quinolone (2), Compound (2) was reacted with different Sulfonyl chloride to yield Sulfonamides [ N-(2-oxoquinolin-1(2H)-yl) methane sulfonamide (3), N-(2-oxoquinolin-1(2H)-yl) Benzene sulfonamide (4) and 4-methyl-N-(2-oxoquinolin-1(2H)-yl) benzene sulfonamide (5) ], while  reaction of  2-(4-methyl-2-oxo-2H-chromen-7-yloxy) acetic acid (8) with different amines yielded compounds [  2-(4-methyl-2-oxo-2H-chromen-7-yloxy)-N-(2-oxoquinolin-1(2H)-yl) acetamide (9) and N-(5-methyl-1,3,4-thiadiazol-2-yl)-2-(4-methyl-2-oxo-2H-chromen-7-yloxy)acetamide (10) ] th

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Publication Date
Sat Dec 18 2021
Journal Name
Egyptian Journal Of Chemistry
Coumarin based-histone deactylace HADC inhibitors
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Coumarins have been recognized as anticancer competitors. HDACis are one of the interesting issues in the field of antitumor research. In order to achieve an increased anticancer efficacy, a series of hybrid compounds bearing coumarin scaffolds have been designed and synthesized as novel HDACis, In this review we present a series of novel HDAC inhibitors comprising coumarin as a core e of cap group of HDAC inhibitors that have been designed, synthesized and assessed for their enzyme inhibitory activity as well as antiproliferative activity. Most of them exhibited potent HDAC inhibitory activity and significant cytotoxicity

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