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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
Fri Mar 25 2016
Journal Name
Oriental Journal Of Chemistry
Synthesis and Antioxidant Ability of New 5-amino-1,2,4-Triazole Derivatives Containing 2,6-dimethoxyphenol
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4-amino-3-(4-(((4-hydroxy-3,5dimethoxybenzyl)oxy)methyl)phenyl)-1,2,4-triazole-5-thione was synthesized by to method the first one from melt reaction of 4-(((4-hydroxy-3,5-dimethoxybenzyl)oxy)methyl)benzoic acid with Thiocarbonyldihydrazide, the second method from convert the corresponded acid hydrazide to potassium 2-(4-(((4-hydroxy-3,5-dimethoxybenzyl)oxy)methyl)benzoyl)hydrazinecarbodithioate salt then react with hydrazine hydrate. Newly Schiff base (7a-7f) were synthesized from reaction the 4-amino-1,2,4-triazol with substituted hydroxybenzaldehyde. The resulting compounds were characterized by IR, 1H-NMR, 13C-NMR, and HRMS data. 2,2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) assays were used to scree

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Publication Date
Tue Feb 12 2013
Journal Name
International Journal Of Engineering Sciences And Research Technology
Synthesis, Characterization of New Azo Compounds and Studies Effect on the Ach Enzyme(Invitro)
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Three azo compounds were synthesized in two different methods, and characterized by FT-IR, HNMR andVis) spectra, melting points were determined. The inhibitory effects of prepared compounds on the activity of human serum cholinesterase have been studied in vitro. Different concentrations of study the type of inhibition. The results form line weaver-Burk plot indicated that the inhibitor type was noncompetitive with a range (33.12-78.99%).

Publication Date
Mon Jun 27 2022
Journal Name
. J Pharm Negative Results
Synthesis, Antioxidant, antibacterial and docking structure of new dihydro-pyrimidine derivatives containing multi phenol
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Newly series of 6,6’-((2-(Aryl)dihydropyrimidine-1,3(2H,4H)-diyl)bis(methylene))bis(2-methoxy phenol) (3a-i) were synthesized from cyclization of 6,6’-((propane-1,3-diylbis (azanediyl)) bis(methylene)) bis(2-methoxyphenol) with several aryl aldehyde in the presence of acetic acid. The newly compounds characterized from their IR, NMR and EIMs spectra. The antioxidant capacity of these compounds screened by utilizing DPPH and FRAP assays. Compounds 3g and 3i exhibited significant antioxidant capability in both assays. Docking study for these compounds as a potential inhibitors of gyrase enzyme were carried out. Compound 3g exhibited significant inhibition with binding free energies (DG) higher than novobiocin. compounds 2, 3a, 3b, 3

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Publication Date
Tue Aug 05 2014
Journal Name
International Journal Of Engineering Sciences & Research Technology
Synthesis and Characterization of Some New Metal Complexes 2-(4-nitrophenyl azo)-2,4- dimethylphenol.
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The Ligand 2-(4-nitrophenyl azo)-2,4-dimethylphenol derived from 4-nitroaniline and 2,4-dimethylphenol was synthesized. The prepared ligand was identified by FT-IR and UV-Vis spectroscopic techniques. Treatment of the ligand with the following metal ions ( CuII , ZnII ,CdII and HgII) in aqueous ethanol with a 1:2 M:L ratio. Characterization of these compounds has been done on the basis of FT-IR and UV-Vis, as well as magnetic susceptibility and conductivity measurements. On the basis of physicochemical data tetrahedral geometries were assigned for the complexes.

Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New Polyimide by Curing Poly Acryloyl Chloride with Different Amides
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The present work involved preparation of new substituted and unsubstituted and poly imides (1-17) using reaction of acryloyl chloride with different amides (aliphatic ,aromatic) in the presence of a suitable solvent and amount tri ethyl amine (Et3N) with heating – the structure confirmation of all polymers were proved using FT-IR,1H-NMR,C13NMR and UV spectroscopy ,thermal analysis (TG) for some polymers confirmed their thermal stabilities . Other physical properties including softening and melting points, PH and solubility of the polymers were also measured

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New Mannich Bases Derived from 7-hydroxy-4-methyl Coumarin
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Coumarin is a natural substance isolated from different plants. It belonges to a group of benzobyrones which consists of a benzene ring joined to a pyrone nucleus. In the present research, a new series of coumarin derivatives were formed. Compound (1) (7-hydroxy-4-methyl Coumarin) was converted into 4-methylquinolin-2(H) derivative (2) by reaction with acetamide, and then reaction of (2) with thiosemicarbazide in ethanol leads to the synthesize of hydrazincarbothioamide derivative (3).The reaction of (3) with ethylchloroacetate in presence of sodium acetate leads to closure ring to get [(1-(5-oxo-2-thioxoimidazolidin-1-ylimino) ethyl)]quinolin-2(1H)-one (4). Mannich bases were prepared through the reaction of (4) with primary

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Publication Date
Sat Jun 20 2020
Journal Name
International Journal Of Pharmaceutical Research
Synthesis , Physicochemical Studies and biological estimation of new mixed ligand complexes from hetrocyclic compounds
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The purpose of this research is to synthesize a new mixed ligand Schiff base complexes of Co(II),Ni(II),Cu(II), Zn(II), Cd(II), and Hg(II),which are formulated from the Schiff base (L) that resulted from orthophathalaldehyde (2-PA) with 4-chloroaniline(4-NA). Diagnosis of prepared Ligand and its complexes is done by spectral methods as 1H–NMR, mass spectrometer, FTIR, UV-Vis, molar conductance, elemental microanalyses, atomic absoption and magnetic susceptibility. The analytical studyofall new complexes has shown octahedral geometries. Organic performance study of ligand Schiff base and its complexes reveals different activities agansit four types of bactria; two gram (+) and two gram (-) .

Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis And Characterization Of Some New Acetylenic Mannich Bases Based On Biphenyl – 4,4 - Dithiol
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One of the most important , compound which have active hydrogen is the compound possessing (thiol group) Biphenyl-4,4-dithiol is agood example utilized in a wide field for preparation mannich bases , avariety of new acetylenic mannich bases have been Synthesized and all proposed structure were Supported by FTIR , 1H – NMR, 13C-NMR , Elemental analysis and microbial study .

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Publication Date
Mon Sep 11 2023
Journal Name
University Of Anbar‎
Synthesis, ‎Characterization and ‎Thermal Study ‎of new aza-‎macrocyclic ligands with ‎some transition metals
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12 membered Schiff base macrocyclic ligands, 6,7,14,15-tetra phenyl-1,2,3,4, 4a,8a, 9,10, 11,12, 12a,16a-dodecahydro dibenzo [b,h] [1,4,7,10] tetraazacyclododecine L1, and 14 membered Schiff base macrocyclic ligands, 6,8,15,17-tetramethyl-1,2,3,4, 4a,7,9a, 10,11,12,13,13a,16,18a-tetra decahydro dibenzo[b,i] [1, 4,8,11] cyclotetradecine tetraaza L2, 7,16-bis(2,4- dichloro benz ylidene)-6,8,15,17-tetra methyl-1,2,3,4, 4a,7,9a, 10, 11,12, 13, 13a,16,18a-tetra deca hydro dibenzo [b,i] [1,4,8,11] tetra azacyclo tetra decine L3 and 6,8,15, 17-tetramethyl-1,2,3, 4,4a,9a,10, 11,12,13,13a,18a-dodecahydro dibenzo [b,i] [1,4,8, 11] tetraazacyclo tetradecine (7,16-diylidene) bis(methanylyli dene) bis (N,N-dimethylaniline) L4 were synthesized by condens

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Publication Date
Wed Jun 30 2004
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Improving the Activity of NiO-NiFe2 Catalyst by Na2O for Phenol Synthesis
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