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Synthesis of New Cephalosporins of Expected Improved Activity and Resistance Against -Lactamases
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The development of new cephalosporins with improved activity against resistant microbes, such as, MRSA (methicillin resistant Staph. aureus), P. aeruginosa, is of high potential. Chemical synthesis of two new series of thiadiazole linked to cysteine (series 1) and cephalosporins containing thiadiazole linked to cysteine through disulfide bond (series 2) were achieved. The chemical structures of the synthesized compounds were confirmed using spectral (FT-IR, 1H-NMR) and elemental microanalysis. The incorporation of privileged chemical moieties, such as, thiadiazole, Schiff base, cysteine and sulfonamide, has been found to have great contribution to the antimicrobial activities. Compounds of series 1 (1b-d), containing a Schiff base or a sulfonamido moiety, showed reasonable activity and were less potent than cephalexin with respect to E. coli and Staph. aureus. The new cephalosporins (series 2) showed remarkable activities on E. coli (62.5-15.6µg/ml) and staph. aureus (31.2-62.5µg/ml) when compared with cephalexin (250 and 125 µg/ml) respectively. Moreover, compounds 1 and 3 showed very promising activity against MRSA (250 and 500µg/ml) respectively. The incorporation of a sulfonamido moiety to the cephalosporin molecule was successfully achieved. This is a very interesting finding which may open a new approach in the synthesis of newer cephalosporins.   

Keywords: Cephalosporins, Cysteine, Schiff base, Sulfonamides, Thiadiazole.

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Publication Date
Thu Apr 20 2023
Journal Name
International Journal Of Biomaterials
Antifungal Activity of Bioactive Compounds Produced by the Endophytic Fungus Paecilomyces sp. (JN227071.1) against Rhizoctonia solani
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Biologically active natural compounds are molecules produced by plants or plant-related microbes, such as endophytes. Many of these metabolites have a wide range of antimicrobial activities and other pharmaceutical properties. This study aimed to evaluate (in vitro) the antifungal activities of the secondary metabolites obtained from Paecilomyces sp. against the pathogenic fungus Rhizoctonia solani. The endophytic fungus Paecilomyces was isolated from Moringa oleifera leaves and cultured on potato dextrose broth for the production of the fungal metabolites. The activity of Paecilomyces filtrate against the radial growth of Rhizoctonia solani was tested by mixing the filtrate with potato dextrose agar medium at concentrations of 15%,

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Publication Date
Thu Apr 20 2023
Journal Name
International Journal Of Biomaterials
Antifungal Activity of Bioactive Compounds Produced by the Endophytic Fungus Paecilomyces sp. (JN227071.1) against Rhizoctonia solani
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Biologically active natural compounds are molecules produced by plants or plant-related microbes, such as endophytes. Many of these metabolites have a wide range of antimicrobial activities and other pharmaceutical properties. This study aimed to evaluate (in vitro) the antifungal activities of the secondary metabolites obtained from Paecilomyces sp. against the pathogenic fungus Rhizoctonia solani. The endophytic fungus Paecilomyces was isolated from Moringa oleifera leaves and cultured on potato dextrose broth for the production of the fungal metabolites. The activity of Paecilomyces filtrate against the radial growth of Rhizoctonia solani was tested by mixing the filtrate with potato dextrose agar medium at concentrations of 15%,

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Publication Date
Sun Mar 31 2024
Journal Name
Plant Science Today
Extraction of Synephrine from Waste Peels of Citrus sinensis and Green Synthesis of Gold Nanoparticles from it against Dermatophytes
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The main object of the current work was to determine the antifungal efficiency of secondary metabolites product called synephrine that extracted from Citrus sinesis peels and the ability of synephrine to biosynthesis gold nanoparticles from HAucl4 which consider environmentally favourable method, then determine their activity against pathogenic human dermatophyte. The identification of synephrine done by Thin layer chromatography (TLC), High Performance Liquid Chromatography (HPLC) and The Fourier Transform Infrared (FTIR). The characterization of gold nanoparticles by using Ultra Violet-Visible Spectroscopy (UV-Vis), Field – Emission Scanning Electron Microscopy (FESEM) and Fourier Transform Infrared (FTIR), confirmed the biosynt

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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
Mon Jan 01 2024
Journal Name
5th International Conference On Biomedical And Health Sciences
Exploiting Vpusm 8 Lytic Phage for The Bio- Control of V. Cholerae: A Novel Approach Against Cholera in The Era of Antibiotic Resistance
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Objective: The purpose of this study was to assess the effectiveness of Vibriophage Universiti Sains Malaysia 8 (VPUSM 8), a bacteriophage that destroys bacteria, in managing the proliferation of Vibrio cholerae, specifically the El Tor serotype, as an alternate therapeutic strategy. Methods: The study entailed subjecting water samples from Kelantan, Malaysia, to reproduce the natural circumstances that promote the growth of V. cholerae. Subsequently, the samples were contaminated with the V. cholerae O1 El Tor Inaba strain and treated using VPUSM 8. The study employed a controlled experimental design, wherein the samples were divided into three groups, each experiencing different treatment methods. Quantifying the number of colony-

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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
Fri Jun 09 2017
Journal Name
Iraqi National Journal Of Chemistry
Synthesis and Characterization of some New Oxazepine Compounds Derived from D-Erythroascorbic Acid
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This search include the synthesis of some new 1,3-oxazepine derivatives have been prepared, starting from reaction of L-ascorbic acid with dry acetone in presence of dry hydrogen chloride afforded the acetal (I). Treatment of the latter with p-nitrobenzoyl chloride in pyridine yielded the ester (II) which was dissolved in (65%) acetic acid in absolute ethanol yielded the glycol (III). The reaction of the glycol (III) with sodium periodate in distilled water at room temperature produced the aldehyde (IV). The compound (V) [4-(1,3-dioxoisoindolin-2-yl)benzoic acid] was synthesized by reaction p-aminobenzoic acid and phthalic anhydride in presence of (gla. CH3COOH). Reaction of compound (V) with thionyl chloride produced [4-(1,3-dioxoisoindoli

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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
    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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