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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 Jun 01 2014
Journal Name
Baghdad Science Journal
Synthesis of Some new 2-(4-Aryliminophenoxy)N-Arylacetamide Via p-hydroxy benzaldehyde.
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Chloroacetamide derivatives (2a-g) have been prepared through reaction of chloroacetyl chloride(1) (which prepared by the reaction of chloroacetic acid with thionyl chloride) with primary aromatic amines and sulfa compounds to afford compounds (2a-g) which then reacted with p-hydroxy benzaldehyde via Williamson reaction to obtaine the new compounds 2-(4-formyl phenoxy)-N-aryl acetamide (3a-g). Finally , compounds (3a-g) will be use as a good synthon to prepare the Schiff bases represented by compounds 2-(4-aryliminophenoxy)-N-arylacetamide (4a-g). through , reaction with some primary aromatic amine. All the prepared compounds were investigated by the available physical and spectroscopic methods.

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Publication Date
Fri Nov 01 2019
Journal Name
Journal Of Global Pharma Technology
Synthesis and Phase Transition Study of New Mesogence Derived from 1, 4-Phenylenediamine
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This work include synthesized and characterization the compound [I] by reaction 1,4-phenylenediamine with chloro acetic acid then this compound reaction with methanol in present sulfuric acid to synthesized ester compound [II] after that reaction with hydrazine hydrate to synthesized acide hydrazide [III] and the later compound reaction with substituted acetophenone[IV]n to synthesized substituted acetophenone hydrazones[V-XI]. In addition synthesized4-formylpyrazole derivatives [XIIXVIII] via cyclisation substituted acetophenone hydrazones [V-XI] with Vilsmeier-Haack reagent DMF/POCl3. The compounds characterized by melting points, FTIR, 1HNMR and mass spectroscopy. The mesomorphic behavior studied by using polarized optical microscopy and

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Publication Date
Tue Jun 01 2021
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Gas Sensor Application of New Composite Based on MWCNTs:CoPc:Metal Oxide
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The synthesis of new substituted cobalt Phthalocyanine (CoPc) was carried out using starting materials Naphthalene-1,4,5, tetracarbonic acid dianhydride (NDI) employing dry process method. Metal oxides (MO) alloy of (60%Ni3O4 40%-Co3O4 ) have been functionalized with multiwall carbon nanotubes (F-MWCNTs) to produce (F-MWCNTs/MO) nanocomposite (E2) and mixed with  CoPc to yield (F-MWCNT/CoPc/MO) (E3). These composites were investigated using different analytical and spectrophotometric methods such as 1H-NMR (0-18 ppm), FTIR spectroscopy in the range of (400-4000cm-1), powder X-rays diffraction (PXRD, 2θ o = 10-80), Raman spectroscopy (0-4000 cm-1), and UV-Visib

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Publication Date
Sat Jun 29 2024
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Characterization of New 5-Fluoroisatin-Chalcone Conjugates with Expected Antimicrobial Activity
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Pathogenic microorganisms are becoming more and more resistant to antimicrobial agents. So the synthesis of new antimicrobial agents is very important. In this work, new 5-fluoroisatin-chalcone conjugates 5(a–g) were synthesized based on previous research that showed the modifications of the isatin moiety led to the synthesis of many derivatives that have antimicrobial activity. 4-aminoacetophenone reacts with 5-fluoroisatin to form Schiff base (3), which in turn reacts with two different groups of aromatic (carbocyclic and heterocyclic) aldehydes 4(a–g) separately to form the final compounds 5(a–g). Proton-nuclear magnetic resonance (¹H-NMR) and Fourier-transform infrared (FT-IR) spectroscopy were used to confirm the chemic

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Publication Date
Sun Jun 07 2015
Journal Name
Baghdad Science Journal
Synthesis, Characterization, Thermal Analysis and Structural Studies of New Complexes with Tetradentate Ligand
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Some new complexes of 4-(5-(1,5-dimethyl-3-oxo-2-phenyl pyrazolidin-4- ylimino)-3,3-dimethyl cyclohexylideneamino) -1,5- dimethyl-2- phenyl -1H- pyrazol -3(2H) –one (L) with Mn(II), Fe(III), Co(II), Ni(II), Cu(II), Pd(II), Re(V) and Pt(IV) were prepared. The ligand and its metal complexes were characterized by phisco- chemical spectroscopic techniques. The spectral data were suggested that the (L) as a neutral tetradentate ligand is coordinated with the metal ions through two nitrogen and two oxygen atoms. These studies revealed Octahedral geometries for all metal complexes, except square planar for Pd(II) complex. Moreover, the thermodynamic activation parameters, such as ?E*, ?H, ?S, ?G and K are calculated from the TGA curves using Coa

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Publication Date
Mon Jan 01 2024
Journal Name
Russian Journal Of Organic Chemistry
Synthesis and Biological Activity of Some New 1,3,4-Oxadiazoles Derived from Carboxylic Acids
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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of New Opioid Analgesic Peptide Analogues to Enkephalin (Leucine- and Methionine-Enkephalin)
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A small number of researches were done in the design and synthesis of enkephalin analogues that are able to resist degradation effect of proteolytic enzymes with good bioavailability and half-lives.Through studying structure activity relationships we tried to incorporate phthalyl group, tryptophan and lysine amino acids in different positions in the basic backbone structure of the naturally occurring opioid Leu5- and Met5- enkephalin, in the hope that such insertion of these amino acids could induce interesting addition in the biological activity of these analogues with enhancement of their bioavailability, in addition to decrease side effects as addiction liability.

These synthesized peptides are:

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    Publication Date
    Mon Mar 22 2010
    Journal Name
    Al- Mustansiriya J. Sci
    Synthesis of New Amides and Schiff Bases derived From 2-Amino-1,3,4- Oxadiazole
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    New compounds of amids [IV]a-e and Schiff bases [V]f-h derived from 2-amino-1,3,4-oxadiazoles [III] were synthesized and characterized by physical and spectraldata.2-Aamino-1,3,4-oxadiazoles was prepared by the action of bromine on acorresponding semicarbazide [II]( which was prepared by reaction of dialdehyde [I]with semicarbazide hydrochloride ) in the presence of sodium acetate , followed byan intramolecular cyclization . (PDF) Synthesis of New Amides and Schiff Bases derived From 2-Amino -1,3,4- Oxadiazole. Available from: https://www.researchgate.net/publication/326679206_Synthesis_of_New_Amides_and_Schiff_Bases_derived_From_2-Amino_-134-_Oxadiazole [accessed Nov 15 2023].

    Publication Date
    Thu Dec 31 2020
    Journal Name
    Iraqi Journal Of Market Research And Consumer Protection
    SYNTHESIS NEW LIQUID ELECTRODES FOR DETERMINATION DOMPERIDONE MALEATE BASED ON A MOLECULARLY IMPRINTED POLYMER: SYNTHESIS NEW LIQUID ELECTRODES FOR DETERMINATION DOMPERIDONE MALEATE BASED ON A MOLECULARLY IMPRINTED POLYMER
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    Liquid electrodes of domperidone maleate (DOMP) imprinted polymer were synthesis based on precipitation polymerization mechanism. The molecularly imprinted (MIP) and non-imprinted (NIP) polymers were synthesized using DOMP as a template. By methyl methacrylate (MMA) as monomer, N,Nmethylenebisacrylamide (NMAA) and ethylene glycol dimethacrylate (EGDMA) as cross-linkers and benzoyl peroxide (BP) as an initiator. The molecularly imprinted membranes were synthesis using acetophenone (APH), di-butyl sabacate (DBS), Di octylphthalate (DOPH) and triolyl phosphate (TP)as plasticizers in PVC matrix. The slopes and limit of detection of l

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    Publication Date
    Wed May 10 2023
    Journal Name
    Journal Of Engineering
    ADAPTIVE CYCLIC PREFIX LENGTH FOR CONVOLUITIONAL CODE OFDM SYSTEM IN FREQUENCY SELECTIVE CHANNEL
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    Orthogonal Frequency Division Multiplexing (OFDM) is one of recent years multicarrier modulation used in order to combat the Inter Symbol Interference (ISI) introduced by frequency selective mobile radio channel. The circular extension of the data symbol, commonly referred to as cyclic prefix is one of the key elements in an OFDM transmission scheme. This paper study The influence of the cyclic prefix duration on the BER performance of an OFDM-VCPL (Orthogonal frequency division multiplexing - Variable Cyclic Prefix Length) system and the conventional OFDM system with frame 64-QAM modulation is evaluated by means of computer simulation in a multipath fading channel. The adaptation of CP is done with respect to the delay spread estimation

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