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Synthesis, Characterization, and Antimicrobial Evaluation of New Ceftriaxone Derivatives
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The present study was designed to synthesize a number of new Ceftriaxone derivatives by its involvement with a series of different amines, through the chemical derivatization of its 2-aminothiazolyl- group into an amide with chloroacetyl chloride, which on further conjugation with these selected amines will produce compounds with pharmacological effects that may extend the antimicrobial activity of the parent compound depending on the nature of these moieties.

Ceftriaxone was first equipped with a spacer arm (linker) by the action of chloroacetyl chloride in aqueous medium and then further reacted with seven different aliphatic and aromatic amines which resulted in the production of the aimed final target products. The syntheses have been carried out following simple methodology in excellent isolated yields.

The structure of the synthesized derivatives has been characterized by elemental microanalysis (CHN), FTIR spectroscopy, and other physicochemical properties. All the final synthesized compounds were screened for their antimicrobial activity against selected microorganisms and showed excellent antibacterial and antifungal activities in comparison to Ceftriaxone, Cephalexin and Fluconazole.

The new Ceftriaxone derivatives have broadened the antimicrobial spectrum of the parent compound in having an extra antifungal activity in addition to its original antibacterial activity.

Keywords: Ceftriaxone, 2-aminothiazole, Antimicrobial activity, Antifungal activity, Ceftriaxone derivatives.

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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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    Crossref
    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
    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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    Scopus
    Publication Date
    Tue Aug 02 2011
    Journal Name
    J. College Of Education / Al-mustansiriya University
    Synthesis and characterization of mixed ligand complexes of some metals with ( L- phenylalanine and nicotinamide)
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    This paper presents the synthesis and study of some new mixed-ligand complexes containing nicotinamide(C6H7N2O) symbolized (NA) and phenylalanine (C9H11NO2)symbolized (pheH)] with some metal ions. The resulting products were found to be solid crystalline complexes which have been characterized by :Melting points, Solubility, Molar conductivity. determination the percentage of the metal in the complexes by flame(AAS), magnetic susceptipibility, Spectroscopic Method [FT-IR and UV-Vis]. The proposed structure of the complexes using program , chem office 3D(2006) . The general formula have been given for the prepared complexes : [M(NA)2(phe)]cl M(II): Mn(II) ,Co(II) , Ni(II) , Cu(II) , Zn(II) , Cd(II) & Hg(II)). NA = Nicotinamide= C6

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    Publication Date
    Mon Aug 01 2016
    Journal Name
    Iraqi Journal Of Science
    Synthesis, Characterization and Study of The Liquid Crystalline Behavior of Four and Six Heterocyclic Compounds
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    The new compounds synthesized by sequence reactions starting from a reaction of 4-hydroxybenzaldehyde with 1,5-dibromo pentane to produce dialdehyde)I( .Then compound )I( reacted with different aromatic amines to give schiff bases )IIIV(,thereafter added acetyl chloride to schiff bases to yield N-acyl derivatives)VVII(.While1,3-diazetine derivatives)VIII-X( were synthesized from the reaction of N-acyl derivatives with sodium azide.The reaction of thiourea with N-acyl compounds led to formation of thiourea derivatives (XI-XIII).Finally, the pyrimidine compounds )XIV-XVI( were synthesized by ring closure reaction of compounds(XIXIII) with diethyl malonate.The synthesized compounds were characterized by measurements of melting points,FTIR,1H-N

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    Publication Date
    Sun Jan 01 2012
    Journal Name
    Al-mustansiriya J. College Of Education
    Synthesis and characterization of mixed ligand complexes of some metals with ( L- phenylalanine and nicotinamide)
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    This paper presents the synthesis and study of some new mixed-liagnd complexes containing nicotinamide(C6H7N2O) symbolized (NA) and phenylalanine (C9H11NO2)symbolized (pheH)] with some metal ions. The resulting products were found to be solid crystalline complexes which have been characterized by :Melting points, Solubility, Molar conductivity. determination the percentage of the metal in the complexes by flame(AAS), magnetic susceptipibility, Spectroscopic Method [FT-IR and UV-Vis]. The proposed structure of the complexes using program , chem office 3D(2006) . The general formula have been given for the prepared complexes :[M(NA)2(phe)]cl M(II): Mn(II) ,Co(II) , Ni(II) , Cu(II) , Zn(II) , Cd(II) & Hg(II) . NA = Nicotinamide= C6H7N2O Phe -

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    Publication Date
    Wed Jun 30 2021
    Journal Name
    Iraqi Journal Of Market Research And Consumer Protection
    SYNTHESIS OF NEW LEVOFLOXACIN SELECTIVE MEMBRANE SENSOR BASED ON MOLECULARLY IMPRINTED POLYMERS.: SYNTHESIS OF NEW LEVOFLOXACIN SELECTIVE MEMBRANE SENSOR BASED ON MOLECULARLY IMPRINTED POLYMERS.
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    Two molecular imprinted polymer (MIP) membranes for Levofloxacin (LEV) were prepared based on PVC matrix. The imprinted polymers were prepared by polymerization of styrene (STY) as monomer, N,N methylene di acrylamide as a cross linker ,benzoyl peroxide (BPO) as an initiator and levofloxacin as a template. Di methyl adepate (DMA) and acetophenone (AOPH) were used as plasticizers , the molecular imprinted membranes and the non molecular imprinted membranes were prepared.  The slopes and detection limits of the liquid electrodes ranged from -21.96 – -19.38 mV/decade and 2×10-4M- 4×10-4M, and Its response time was around 1 minute, respectively. The liquid  electrodes were packed with 0.1 M standar

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    Publication Date
    Fri Sep 05 2008
    Journal Name
    Journal Of Kerbala University
    Synthesis of New type of tetrazoles starting from D-ribose
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    This work includes synthesis of sugar tetrazole derivative, D-ribose reacted with acetone in the presence of sulfuric acid H2SO4 to give 2, 3-O-isopropylidene-D-ribose (1). The Aldol condensation of (1) with formaldehyde in methanolic K2CO3 solution gave 2-hydroxymethyl (2, 3-O-isopropylidene-D-ribose)(2). Which was tosylated by Tosyl chloride in pyridine to yield compound (3), SN2 reaction of (3) with sodium cyanide in DMSO afforded compound (4). The [2+ 3] cycloaddition reaction of (4) with sodium azide gave the targeted compound (5). All prepared compounds have been characterized by: TLC, Specific rotation, Microelemental analysis and [FTIR and 1 H NMR spectroscopy]

    Publication Date
    Wed Oct 04 2023
    Journal Name
    History Of Medicine
    Theoretical Biological Activities and Docking studies of new amino-acids Derivatives of Oseltamivir for The Treatment of Coronavirus Disease 2019
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    Antiviral medications may be the best choices for COVID-19 treatment until particular therapeutic treatments become available. Tamiflu (oseltamivir) is a neuraminidase inhibitor licensed for the management and defense against influenza types A and B. Oseltamivir-based medication combinations are currently being used to treat COVID-19 patients who also have the new coronavirus 1 SARS-CoV-2. 1 Oseltamivir administration was related with a less time spent in the hospital, quicker recovery 1 and discharge, and a decreased mortality rate. Docking is a modern computational method for identifying a hit molecule by assessing the binding ability of molecular medicines within the binding target pocket. In this work, we chose 21 ligand compounds that

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    Publication Date
    Sun Jun 01 2025
    Journal Name
    Chemical Review And Letters
    Synthesis, structural characterization, biological evaluation and industrial application of (E)-4-((5-chloro-2-hydroxyphenyl)diazenyl)-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one and its metal complexes
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    The reaction of 1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one with one equivalent of 4-chlorophenol by coupling reaction afforded (E)-4-((5-chloro-2- hydroxyphenyl)diazenyl)-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one. Then azo ligand was characterize using spectroscopic studies ( FTIR,UV-Vis, 1H and 13CNMR, Mass) also micro-elemental analysiz (C.H.N.O). Transition metal chelation with Co(II), Ni(II), Cu(II), and Zn(II) was investigated, revealing 1:2 metal-to-ligand stoichiometry with octahedral geometry. The biological, and industrial application for the azo ligand and it is complexes were evaluated, demonstrating antimicrobial activity against bacterial and fungal strains, with the Zn(II) complex exhibiting superior inhibition. Additionally,

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