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Synthesis of Triazolo and Pyrazolo Derivatives of Quinoline Nucleus

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
Sun Apr 30 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Study Biological Activity of Some New Isoxazoline and Pyrazoline derivatives

   This work involves synthesis of novel Schiff bases derivatives contining isoxazoline or pyrazoline units starting with chalcons . 4-Aminoacetophenone was reacted with 3-nitrobenzaldehyde in basic medium giving chalcone [I] by claisen-schemidt reaction. The chalcone [I]  was reacted with hydroxylamine hydrochloride giving isoxazoline [II]  in basic medium. The chalcone [I] could also react with hydrazitne hydrate to give pyrazoline [III]  . The novel Schiff bases with structural formula [IV] and [V] were prepared by the reaction of amino compounds ; isoxazoline [II] and pyrazolines [III] with p-substituted aldehydes or p-subsituted ketones, respectively in dry benzene using drops of glacial acetic acid as a cat

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Publication Date
Thu Dec 29 2016
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of New Symmetrical Pyromellitdiimide Derivatives and Their Amic Acids

               The new symmetry pyromellitdiimide [VII]a-c,n  were synthesized by two-step reactions from the corresponding pyromellitic dianhydride . A new symmetrical amic acid [VI]a-c,n was synthesized by the reaction of pyromellitic dianhydride with different heterocyclic amines in dry acetone . The second reaction step includes  intramolecular cyclization of amic acid in the presence of  sodium acetate -acetic anhydride system at 850C. Structures  of  the synthesized compounds have been ascertained by their melting points , C.H.N analysis , UV-Vis, FTIR and 1HNMR spectroscopy.

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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 of new derivatives of Ceftazidime as possible Prodrugs

Five new ceftazidime derivatives were designed and synthesized in an attempt to improve the acid stability and may increase the spectrum of ceftazidime. The synthesized compounds included;  Schiff base of ceftazidime (compound 1), ceftazidime lysine amide Schiff base (compound 2), ceftazidime lysine amide (compound 3), ceftazidime-di-lysine amide Schiff base (compound 4) and ceftazidime-di-lysine amide (compound 5). New ceftazidime derivatives were successfully prepared characterized and identified using spectral and elemental microanalysis (CHNS) analyses and the results comply with the calculated measurements.

Compounds 1 and 2 were subjected to a stability study in phosphate buffer (0.2M, pH 7.4) and in KCl/HCl buffer (0.

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Publication Date
Mon Mar 15 2021
Journal Name
Egyptian Journal Of Chemistry
Synthesis and Characterization of some Tetrazole Derivatives and Evaluation of their Biological Activity

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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

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
Fri Mar 01 2013
Journal Name
Chemistry And Materials Research
Synthesis and Characterization of New Derivatives of Thiazole with Liquid Crystalline properties

A new two series of liquid crystalline Schiff bases containing thiazole moiety with different length of alkoxy spacer were synthesized, and the relation between the spacer length and the liquid crystalline behavior was investigated. The molecular structures of these compounds were performed by elemental analysis and FTIR, 1HNMR spectroscopy. The liquid crystalline properties were examined by hot stage optical polarizing microscopy (OPM) and differential scanning calorimetry (DSC). All compouns of the two series display liquid crystalline nematic mesophase. The liquid crystalline behaviour has been analyzed in terms of structural property relationship

Publication Date
Sat Apr 23 2022
Journal Name
Research Journal Of Pharmacy And Technology
Synthesis, and Antimicrobial Evaluation of New hydrazone Derivatives of (2,4-dinitrophenyl) hydrazine

In this work, novel compounds of hydrazones derived from (2,4-dinitrophenyl) hydrazine were synthesized. Benzamides derivatives and sulfonamides derivatives were prepared from p-amino benzaldehyde. Then these compounds were condensed with (2,4-dinitrophenyl) hydrazine through Imine bond formation to give hydrazones compounds. The compounds were characterized using FT-IR (IR Affinity-1) spectrometer, and 1HNMR analyses. The majority of the compounds have a moderate antimicrobial activity against “Gram-positive bacteria staphylococcus Aureus, and staphylococcus epidermidis, Gram-negative bacteria Escherichia coli, and Klebsiella pneumoniae, and fungi species Candida albicans” using concentrations of 250 µg\ml.

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Publication Date
Tue Jan 01 2019
Journal Name
Journal Of Global Pharma Technology
Synthesis of New Derivatives of Cephalexin with Isatin and Glycine Schiff Bases

Objectives: Two derivatives of cephalexin were synthesized by reaction with isatin-glycine Schiff base and bromoisatin-glycine Schiff base separately. Methods: Cephalexin was linked through the amine group to isatin glycine and bromoisatin glycine Schiff bases by amide bond formation. Results: These derivatives were characterized by FT-IR, H-NMR, elemental CHN analysis and then tested for their antimicrobial activity compared to cephalexin against gram-positive, gram-negative bacteria and Candida albicans fungi. Conclusion: The two compounds showed better activity against Staphylococcus aureus, compound 3b is more active against Escherichia coli, and compound 3a is more active against Klebsiella pneumonia.

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Publication Date
Sun Jun 02 2013
Journal Name
Baghdad Science Journal
Synthesis and Characterizationof Some New Phenolic Schiff Bases Derivatives

Starting from bis (4,4'-diamino phenoxy) ethan(1), a variety of phenolicschiff bases (methylolic, etheric, epoxy) derivatives have been synthesized. All proposed structure were supported by FTIR, 1H-NMR, 13C-NMR Elemental analysis, some derivatives evaluated by thermal analysis (TGA).

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis of New Some Imidazole Derivatives Containing ?-Lactam Ring

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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