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bijps-386
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
Wed Jun 25 2025
Journal Name
Iraqi Journal Of Pharmaceutical Sciences
Modified Polyvinyl Alcohol Containing New Imides / Iron Oxide Nanoparticles :Synthesis , Characterization and  Biological Evaluation
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A series of new imides compounds[1-4] were synthesized from reaction of tetrachlorophthalic anhydride or nitro phthalic anhydride or malic anhydride or Succinic anhydride  with  4-amino benzene thiol under fusion conditions. Chloroacetic acid has been added after compounds [1-4] reacted with distilled H2O and Na2CO3, producing compounds [5-8]. In benzene, compounds [5-8] also interacted with the thionyl chloride to produce [9-12]. Poly (vinyl alcohol) was chemically modified by reacting PVA with compounds [9-12] and dimethyl formamide to produce compounds [13-16]. Iron oxide nanoparticles (IONPs) are mixed with modified PVA [13-16] to create nanocomposites [17-20]. Spectral and analytical data from synthesized compounds, such as 1

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Publication Date
Mon Dec 05 2022
Journal Name
Baghdad Science Journal
Heavy Metal Complexes of 1, 2, 3-Triazole derivative: Synthesis, Characterization, and Cytotoxicity Appraisal Against Breast Cancer Cell Lines (MDA-MB-231)
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     New chelating ligand derived from triazole and its complexes with metal ions Rhodium, Platinum and Gold were synthesized. Through a copper (I)-catalyzed click reaction, the ligand produced 1,3-dipolar cycloaddition between 2,6-bis((prop-2-yn-1-yloxy) methyl) pyridine and 1-azidododecane. All structures of these new compounds were rigorously characterized in the solid state using spectroscopic techniques like: 1HNMR, 13CNMR, Uv-Vis, FTIR, metal and elemental analyses, magnetic susceptibility and conductivity measurements at room temperature, it was found that the ligand acts as a penta and tetradentate chelate through N3O2, N2O2, and the geometry of the new complex

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Publication Date
Mon Dec 05 2022
Journal Name
Baghdad Science Journal
Heavy Metal Complexes of 1, 2, 3-Triazole derivative: Synthesis, Characterization, and Cytotoxicity Appraisal Against Breast Cancer Cell Lines (MDA-MB-231)
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     New chelating ligand derived from triazole and its complexes with metal ions Rhodium, Platinum and Gold were synthesized. Through a copper (I)-catalyzed click reaction, the ligand produced 1,3-dipolar cycloaddition between 2,6-bis((prop-2-yn-1-yloxy) methyl) pyridine and 1-azidododecane. All structures of these new compounds were rigorously characterized in the solid state using spectroscopic techniques like: 1HNMR, 13CNMR, Uv-Vis, FTIR, metal and elemental analyses, magnetic susceptibility and conductivity measurements at room temperature, it was found that the ligand acts as a penta and tetradentate chelate through N3O2, N2O2, and the geometry of the new complexes are identified as octahedral for (Rh & Pt) complexes a

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Publication Date
Sun Jun 30 2019
Journal Name
Journal Of Global Pharma Technology
Synthesis, Spectral and Antibacterial Activity of Mixed Ligand from Lanthanium (III) Complexes of Schiff Base Ligand with Some Amino Acids
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In this work, lanthanium (III) complexes were synthesized using by Schiff base ligand (L) derived from benzaldehyde and o-aminoaniline with five amino acids (AA) from glycine (Gly), L-alanine (Ala), L-valine (Val), L-asparagine (Asp) and DL- phenylalanine (Phe). The Schiff base ligand has been characterized by elemental analysis, (MASS, FTIR, 1HNMR, 13CNMR, UV-VIS) electronic spectra. The structures of the new complexes have been described of analysis of elements, molar conductivity, (UV-Vis electronic, FTIR, mass) spectra also magnetic moment. The molar conductivity values of the complexes indicat this every of complexes are electrolytes and other analytical studies reveal octahedral geometry for La (III) ion. The Schiff base ligand, five

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Publication Date
Sun Jul 01 2018
Journal Name
Journal Of Global Pharma Technology
Preparation, Characterization and Biological Activity of New Derivatives of 3-Cyclic Oxazepine, 3-Cyclic Lactam and 3- Aminomethyl Imidazo (1, 2-a) Benzthiazol
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In this work a series of fourteen new compounds were synthesized. Compound [1] was formed from the reaction of 2-aminobenzothiazole and p-bromophenacyl bromide. Aldehyde group [2] was obtained from the reaction of compound [1] with pocl3 in presence of DMF and CHCl3 .After that shiff bases have been synthesized from the reaction of compound [2] with different aromatic amine to give new shiff bases [3- 5]. These new shiff bases have been reduced to their corresponding amine [6-8] by means of sodium borohydride. Then reaction of shiff bases [3-5] with phenyl isocyanate gives 3-cyclic lactam derivatives [9-11]. 3-cyclic Oxazepine derivatives [12-14] were obtained by reaction of shiff bases [3-5] with succinic anhydride. These new formed co

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Publication Date
Tue May 06 2014
Journal Name
Plos One
Gastroprotective Activity of Ethyl-4-[(3,5-di-tert-butyl-2-hydroxybenzylidene) Amino]benzoate against Ethanol-Induced Gastric Mucosal Ulcer in Rats
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The study was carried out to determine the cytotoxic, antioxidant and gastro-protective effect of ethyl-4-[(3,5-di-tert-butyl-2-hydroxybenzylid ene)amino] benzoate (ETHAB) in rats.

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Publication Date
Wed Jan 01 2020
Journal Name
International Journal Of Pharmaceutical Research
Synthesis, characterization and bioactivity study of mixed-lig and complexes with some metal ions for new dithiocarbamate,3-aminophenol
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Publication Date
Fri Jan 01 2016
Journal Name
Ibn Al-haitham Jour. For Pure & Appl. Sci.
Synthesis and Characterization of Some New Mixed- Ligand Complexes Containing Schiff Base and 3-Picoline with Some Metal Salts
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Some metal ions (Mn+2, Co+2, Ni+2, Cu+2,Zn+2 and Cd+2) complexes of quodridentats Schiff base derived from (2-hydroxy benzaldehyde and 4,4'-methylenedianiline as primary ligand and 3-picoline (3-pic) secondary ligand have been synthesized and characterized on the basis of their 1H ,13C-NMR, FT-IR, UV-Vis spectroscopy, conductivity measurements, elemental analysis, and magnetic moments, metal to ligands ratio in all complexes has been found to be (1:1:2) (M:Schiff base:3-pic), Schiff base behaves as neutral tetra dentate ligand with (N2,O2) system from the results obtained, the following general formula has suggested for the prepared complexes [M+2(2-mbd)(3-pic)2] and octahedral stereochemistry, Where M+2 = (Mn , Co , Ni , Cu , Zn and Cd), 2

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Publication Date
Sun Jun 13 2021
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization and Anticorrosion Studies of New Co(II), Ni(II), Cu(II), and Zn(II) Schiff Base Complexes
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The research included preparation of new Schiff base (L) by two steps: preparation of precursor [bis(2-formyl-6-methoxyphenyl) succinate] (P) by reacting (3-methoxy salicyl aldehyde) with (succinoyl dichloride) as first step then react the prepared precursor (P) with (ethanethioamide) to have the new Schiff base [bis(2-((ethane thioyl imino) methyl)-6-methoxy phenyl) succinate] (L) as second step. Characterized compounds based on Mass spectra, 1 H, 13CNMR (for ligand (L)), FT-IR and UV spectrum, melting point, molar conduct, %C, %H, and %N, the percentage of the metal in complexes %M, magnetic susceptibility, while study corrosion inhibition (mild steel) in acid solution by weight loss. These measurements proved that by (Oxygen, Nitrogen, a

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Publication Date
Sun May 23 2010
Journal Name
Ibn Al- Haitham J. Fo R Pure & Appl. Sc I
Synthesis, Spectroscopic and Dyeing Performance Studies of Some New Heterocyclic Azo Dyes and Their Complexes with Selected Metal Ions
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Coupling reaction of m-and p- amino acetop henone and p-amino benzoic acid with (LHistidine) gave the new bidentate azo ligands (L1, L2 and L3). The prepared ligands were identified by FT-IR, UV-Vis, 1HNMR and GC- mass sp ectroscopic technique. Treatment of the prepared ligands with the following metal ions (CoII, NiII, CuII, ZnII, CdII and HgII) in aqueous ethanol with a 1:2 M:L ratio and at optimum pH, yielded a series of neutral complexes of the general formula [M (L)2 Cl2]. The prepared complexes were characterized by using flame atomic absorption, FT-IR, UV-Vis and 1HNMR spectroscopic methods as well as magnetic susceptibility and conductivity measurements. Chloride ion content was also evaluated by (Mohr method). The nature of the com

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