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Synthesis of new Schiff bases and nucleoside analogues derivatives derived from D-Glucose and their biological activity study
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Inthis study new derivatives of Schiff bases and nucleoside analogues have been synthesized from the starting material D-glucose after a series of reactions. Derivative 1 was prepared from D-glucose then react with P-bromoacetophenone gave derivative 2 was reacted with dimethyl sulfoxide and acetic anhydride for dehydration a molecule of water gave 3. The spiro ring was prepared at 3-position from the reaction of 3 derivative with 1-phenyl-2–thioureagave 4. The protection group at 1 position was removed by using acetic acid fllowed by periodate oxidation to obtain 6. Reaction of 6 with hydrazide derivative at once and dtriazole derivative at another gave 8 and 9 respectively. Compound 6 was reduced to gave derivative 7. The 1-hydroxylgroup was protected with benzoyl group by using benzoyl chloride to give the derivative 10. Derivative 10 treatment with a mixture of trifluoroacetic anhydride and acetic acid followed by the reaction with trifluoroacetic anhydride gave derivative 11. When derivative 11 treated with silylated uracil derivative the nucleoside analogue 12 was obtained when 11 allowed to react with mercuric theophylline salt in dry xylene, the nucleoside analogue 13 was obtained. The free nucleoside 14 and 15 were obtained when 12 and 13 were allowed to react with sodium methoxide in ethanol respectively. Compounds 8, 9, 14, 15 were exhibited biological activity against E-coli bacteria. Compound 9 exhibited higher degree of activity than the others

Publication Date
Fri Sep 22 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis A.nd Study The Biological Activity of Some Schiff-Bases Derived F,rom 2- Aminothiazole or 2-Aminobenzothiazole and Vanillin Derivatives
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Two  series    of   1,n-alkylene    glycol   di [4{N(T-thiazolylazo­

nrethinyl)}2-metho y]     phenyl     ether     and     I ,n-alkylene      glycol di[4{N(r-benzo-thiazolylazomethinyl)}2-methoxy]phenyl ether were synthesize-d via rea tions  2-aminothiazole and  2-aminobenzothiazole with  dialdehyde • (which  are synthesized  from  .reaction  vanil.lin with

l ,n-dibromo   or   ehloro.   alkane   in  the   basic   me'dia   )   .  &nb

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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
Mon Jul 04 2022
Journal Name
Al Mustansiriyah Journal Of Pharmaceutical Sciences
Bis-Schiff Bases of Isatin Derivatives Synthesis, and their Biological Activities: A Review
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Isatin is a heterocyclic molecule that belongs to one of the most important classes of organic compounds known as indolines. Isatin, isatin analogs, and their Schiff bases have recently attracted a lot of attention in medicinal chemistry. Isatin, itself, shows various biological activities such as antiviral, anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, and anticonvulsant. Bis- Schiff bases containing isatin moiety have been known to possess a wide spectrum of pharmacological activities. This review offers up-to-date information on the most active isatin bis-Schiff bases, which would include anticancer, antimicrobial, antiviral, anticonvulsant, anti-inflammatory, and analgesic activities. These observations c

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Publication Date
Mon Jul 04 2022
Journal Name
Al Mustansiriyah Journal Of Pharmaceutical Sciences
Bis-Schiff Bases of Isatin Derivatives Synthesis, and their Biological Activities: A Review
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Isatin is a heterocyclic molecule that belongs to one of the most important classes of organic compounds known as indolines. Isatin, isatin analogs, and their Schiff bases have recently attracted a lot of attention in medicinal chemistry. Isatin, itself, shows various biological activities such as antiviral, anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, and anticonvulsant. Bis- Schiff bases containing isatin moiety have been known to possess a wide spectrum of pharmacological activities. This review offers up-to-date information on the most active isatin bis-Schiff bases, which would include anticancer, antimicrobial, antiviral, anticonvulsant, anti-inflammatory, and analgesic activities. These observations c

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Publication Date
Fri Jan 05 2018
Journal Name
Journal Of Pharmaceutical Sciences And Research
Synthesis of New Nucleoside Analogues From 3,5-Disubstituted Pyrazoline
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n this work, a series of new nucleoside analogues (β-glucose liked to pyrazoline moiety) was synthesized. In the beginning, chalcone [1-3] was formed from the reaction of acetophenone and benzaldehyde derivatives in the presence of sodium hydroxide. Pyrazolines [4-6] were obtained from the reaction of the prepared chalcones and hydrazine hydrate in the presence of ethanol absolute. These pyrazolines were treated with β-glucose pentaacetate to afford a series of desirable protected nucleoside analogues [8-10]. After that hydrolysis of protected nuclioside analogues in sodium methoxide gave free nucleoside analogues [11-13]. These new formed compounds were diagnosed by 13C-NMR and 1H- NMR for some of them and FT-IR spectroscopy.

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Publication Date
Wed Aug 02 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis of 3-C-Spiro Ring Nucleoside Analogues, of Possible Biological Activity
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In this study, new derivatives of 3-C-spiro ring nucleoside analogues were synthesized. The structures of these derivatives were characterized by infrared spectroscopy,1HNMR (some of them) and elemental analysis. The nucleoside derivatives were tested for inhibition of E-coli and were all found to be active.

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Publication Date
Tue Mar 15 2016
Journal Name
International Journal Of Pharmacy And Pharmaceutical Sciences
SYNTHESIS, CHARACTERIZATION AND PRELIMINARY ANTIMICROBIAL EVALUATION OF NEW SCHIFF BASES OF AMPICILLIN AND AMOXICILLIN DERIVED FROM ISATIN DERIVATIVES
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Objectives: Six different Schiff bases were synthesized from ampicillin and amoxicillin with isatin, 5-bromoisatin, and 5-nitroisatin. Methods: Ampicillin and Amoxicillin are linked directly through their α-amino groups to the acyl side chain with isatin and isatin derivatives by nucleophilic addition using glacial acetic acid as a catalyst. Results: chemical structures of these Schiff bases were confirmed using FTIR, 1H NMR and elemental microanalysis. The antibacterial activity was evaluated by measuring minimum inhibitory concentration (MIC) values and showed various degrees of antibacterial activities when compared with parent drugs. Compounds 1a and 2b, which are the Schiff bases of ampicillin and amoxicillin with isatin, showed very

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Publication Date
Thu May 17 2018
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis, Characterization and Study of Biological Activity of Some New Schiff Bases, 1, 3-Oxazepine and Tetrazole Derived from 2, 2 di thiophenyl Acetic Acid
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In this study new derivatives of Schiff bases 5-8, 1, 3-oxazepine 9-16 and tetrazoles 17-19 have been synthesized from the new starting material 1 which has synthesized the reaction of one mole of dichloro acetic acid and two moles of thiophenol, the esters 2-3 were synthesized from the reaction of compound 1 with methanol or ethanol respectively in the presence of H2SO4 as catalyst then 2, 2-dithiophenylaceto Hydrazide 4 were synthesized from the reaction of 2 or 3 with hydrazine hydrate 80%, Schiff bases 5-8 were synthesized from the reaction of 4 with appropriate aldehyde or ketone. Treatment of Schiff bases with maleic and phathalic anhydride in dry benzene to give 1, 3-oxazepen derivatives 9-16 and with sodium azide in tetrahydrofuran

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Publication Date
Tue Nov 01 2022
Journal Name
Chemical Methodologies
Synthesis and Characterization of New Substituted Coumarin Derivatives and Study Their Biological Activity
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New substituted coumarins derivatives were synthesized by using nitration reaction to produce different nitro coumarin isomers which were separated from these isomers by using different solvent, and the reduction of nitro compounds was done to give corresponding amino coumarins. Temperature and reaction time of reaction were very important factors in determining the most productive nitro isotopes. A low temperature for three hours was sufficient to give a high product of a compound 6-nitro coumarin while increasing the temperature for a period of twenty-four hours that gave a high product of 8-nitro-coumarin. The synthesized compounds were confirmed by FT-IR,1 H-NMR, and13 C-NMR spectroscopy and all final compounds were tested for their ant

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Publication Date
Fri Aug 06 2021
Journal Name
Research Journal Of Pharmacy And Technology
Synthesis, Antimicrobial evaluation and Docking study of new Schiff bases of benzo[d]oxazol-5-amine derivatives.
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Objective: Benzoxazole derivatives have antifungal, anticancer, antibacterial, and anticonvulsant function. Encouraged by this comment, we agreed to synthesize new Benzoxazole compounds connected to the bases of Schiff's. Methods: 2,4-diaminophenol (1) was prepared by the reaction of 2,4-dinitrophenol and sodium dithionate. Compound (1) reacted with either acetic acid to afford compound (2) or with formic acid to afford compound (3). The Schiff bases were preparation from the reaction condensing reaction of compound (2) or (3) and aromatic aldehydes or ketone; [p-nitrobenzaldehyde, p-hydroxybenzaldehyde, p-chlorobenzaldehyde, p-bromoacetophenone and terephthaldehyde]. Results: FTIR and 1H-NMR spectroscopy characterized all of the pr

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