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Synthesis of New Cyclic Amines-Linked Metronidazole Derivatives as Possible Prodrugs
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         Certain cyclic amine derivatives of metronidazole via acetate spacer were prepared. Cyclic amines used are piperidine and piperazine to improve the physicochemical properties and reduce some of metronidazole side effects. This is believed to be done by modification of its structural features to get prodrugs with improved properties over that of metronidazole. The present work includes esterification of metronidazole with choroacetic acid, N-alkylation of the cyclic amines by the halogenated ester and characterization of their structures by spectral(UV and IR) and elemental(CHN)analysis.The melting points, degree of solubilities and partition coefficients were also determined. Both metronidazole-piperazine and metronidazole-piperidine derivatives have different structural and physicochemical properties that may be excellent to diminish problems associated with metronidazole.

Key words: Metronidazole, chloroacetate, prodrug.

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Publication Date
Sun Dec 14 2014
Journal Name
Molecular Crystals And Liquid Crysta
Synthesis and Mesomorphic Behavior of Two New Homologous Series Containing Azobenzene and 1,3,4-Oxadiazole Units
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Two new nonsymmetrical mesogenic homologous series of terminal substituent ether (series [Vn]) and carboxy (series [VIn]) incorporating azobenzene and 1,3,4-oxadiazole group were synthesized. Both series have been All compounds thus isolated were purified and characterized by elemental analysis, Fourier Transform Infrared Spectroscopy, 1H NMR, along with thermal analysis and texture observation using Differential Scanning Calorimetry (DSC) and Polarizing Optical Microscopy (POM), respectively. All compounds of the first series exhibited liquid crystalline properties. The homologues [V1]-[V3] display a nematic mesophase, the compounds [V4]-[V7] exhibit a dimorphism behavior, nematic (N) and smectic A (SmA) mesophases, the compounds [V8] and

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Publication Date
Thu Jan 15 2015
Journal Name
Journal Of Education For Pure Science
Synthesis and Characterization of New Conjugated Systems Derived from Piperazine-2,5-dione with antimicrobial screening
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Publication Date
Mon May 18 2009
Journal Name
Journal Of Global Pharma Technology
Synthesis, Thermal and Electrochemical Properties of Four New Bis Oxadiazole Copolymers Based on Azo Monomer
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Four new copolymers were synthesized from reaction of bis acid monomer 3-((4-carboxyphenyl) diazenyl)-5-chloro-2-hydroxybenzoic acid with five diacidhydrazide in presence of poly phosphoric acid. The resulted monomers and copolymers have been characterized by FT-IR, 1H-NMR, 13C-NMR spectroscopy as well as EIMs technique. The number averages of molecular weights of the copolymers are between 4822 and 9144, and their polydispersity indexes are between 1.02 and 2.15. All the copolymers show good thermal stability with the temperatures higher than 305.86 C when losing 10% weight under nitrogen. The cyclic voltammetry (CV) measurement and the electrochemical band gaps (Eg) of these copolymers are found below 2.00 ev.

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Publication Date
Tue Mar 24 2009
Journal Name
The 11th Scientific Conference Of Foundation Of Technical Education
Synthesis and Characterization of Some Metal Ions (CoII,NiII,CuII,ZnII) with New Azo Ligand
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Publication Date
Sat Jul 01 2023
Journal Name
Journal Of Nanostructures
Synthesis and Evaluation Biological Activity of Some New Polymers Derived From 3,3’-dimethoxybiphenyl-4,4’-diamine
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In this study, synthesis of polymer Nanocomposites through the blending of prepared polymers with polyvinyl alcohol (a synthetic polymer) or chitosan (a natural polymer) then mixed with nano oxide silica by many steps. The new compound [I] was obtained via reaction of 3,3’-dimethoxybiphenyl-4,4’-diamine as starting material with malic anhydride in DMF then treatment with ammonium persulfate (NH4 )2 S2 O8 (as the initiator) in order to produce polymer [II]. Also, we prepared new polymers [III-V] by using the same starting material (3,3’-dimethoxybiphenyl-4,4’-diamine) with glutaric acid or adipic acid or isophthalic acid in DMF and pyridine. In this study, new polymer blending [VI-IX] and [X-XIII] were synthesized from a prepared pol

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Publication Date
Sun Jun 16 2013
Journal Name
International Journal For Sciences And Technology
Synthesis and Characterization of Some New Thiazine-4-Ones Containing 1, 3, 4-Thiadiazole Moiety
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Small ring heterocycles containing nitrogen and sulfur have been under investigation for a long time because of their important medicinal properties. Among the wide range of heterocycles explored to develop pharmaceutically important molecules, thiadiazoles had played an important role in medicinal chemistry. A survey of literature had shown that compounds having thiadiazole nucleus possess a broad range of biological activities such as anti-inflammatory (1), antibacterial (2), and antifungal activities (3). Thiazine-4-one and their derivatives are import classes of compounds in organic and medicinal chemistry. The thiazine-4-one ring system is a core structure in various synthetic pharmaceutical agents, displaying a broad spectrum of biolo

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis and Characterization of Some New Nucleoside Analogues from Substituted Benzimidazole via 1,3-Dipolar cycloaddition
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This paper includes the synthesis of some new nucleoside analogues starting with 2-substituted benzimidazole derivative (7-9), that synthesized by condensation of O-phenylenediamine with p-chloro benzaldehyde and two substituted benzoic acid , which on nucleophilic substitution with propargyl bromide gave a new N-substituted compounds (10-12). D-Fructose and D-galactose were chosen as a sugar moiety which were protected, brominated and azotated to give azido sugars (5) and (6), then they were subjected to 1,3-dipolar cycloaddition reaction with N-substuted compounds afforded bloked nucleoside analoges (13-16), which after hydrolysis gave our target the free nucleoside analogues (17-20). All prepared compounds were identified by FT-IR

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Publication Date
Wed Jan 01 2020
Journal Name
Egyptian Journal Of Chemistry
Synthesis, Charecterization and Antibacterial Study of New Glyoxilic Acid and Its (N2O4) MnII Ion Complex
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THE Schiff base reaction played an important role of the condensation reaction between 2-aminophenol and Glyoxylic acid in the presence of calculated amounts of KOH as a catalyst. The reaction has been carried out in ethanol under reflux and stirring condition for 3.5 hrs. All syntheses were carried out under hydrogen gas forming a new potassium (E)-1-hydroxy-2-(2-hydroxyphenylimino)ethanolate ligand type [NO2]. The ligand of the general formula K2[Mn(L2)] type and its Mnп complex K2[Mn(N2O4)] type, has been characterized by spectroscopic methods (F.T-I.R. and U.V-Vis.), elemental analysis (C.H.N) metal content, magnetic susceptibility measurement, Thin-layer chromatography (T.L.C), X-RD powder diffraction, 1H-NMR, 13C-NMR molar conductanc

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Publication Date
Mon Mar 27 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of New B-adrenoceptor Blocking Agent Including 1,3,4 Thiadiazole with Expected Adrenoceptor Blocking Activity
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β-Adrenergic blocking agents, mostly comprising of β-amino alcohols, are of pharmaceutical significance and have received major attention due to their utility in the management of cardiovascular disorders including hypertension, angina pectoris, cardiac arrhythmias and other disorders related to the sympathetic nervous system. Most compounds available for clinical use belong to the aryloxypropanolamine series, which is considered the second generation of β-blocking agents. The present study includes the synthesis of compounds with an N-substituted oxypropanolamine moiety attached to the 1, 3, 4-thiadiazole derivatives. According to this information, eight compounds were synthesized and characterized by IR spectra and elemental m

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Publication Date
Wed Jun 24 2020
Journal Name
Systematic Reviews In Pharmacy
Synthesis, Characterization and Spectroscopic Study of New Metal Complexes form Heterocyclic Compounds for Photostability Study
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In present project, new Schiff base of 4, 4'- (((1E, 1'E)-1,4-.phenylenebis- (methane-ylylidene))-bis-(azane-ylylidene)) bis-(5-(4-chlorophenyl) -4H -1,2,4-triazole-3-thione) (L3) has been synthesized by condensation of 4-amino-5-(4-chlorophenyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione with benzene-1,4-dicarboxaldehyde. The new asymmetrical Schiff base (L3) used as a ligand to synthesize a new complex with Co(II), Ni(II), Cu(II), Pd(II), and Pt(IV) metal ions by 1:2 (Metal: ligand) ratio. New ligand and their complexes have been exanimated and Confirmed by Fourier-transform infrared (FT-IR), Ultraviolet-visible (UV-visible), Proton nuclear magnetic resonance (1HNMR), carbon13 nuclear magnetic resonance (13CNMR), carbon-hydrogen nitrogen sulf

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