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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
Sat May 27 2017
Journal Name
Journal Of Pharmaceutical Sciences And Research
Synthesis, Preliminary Antimicrobial Evaluation and Molecular Docking of new Schiff bases of Ceftizoxime
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Schiff bases of Ceftizoxime sodium were synthesized in an attempt to improve the antimicrobial spectrum of Ceftizoxime. Aminothiazole ring of Ceftizoxime is linked directly through an imino group to different aromatic aldehydes reacted by nucleophilic addition using trimethylamine (TEA), as a catalyst and refluxed in methanol. The antimicrobial activity was evaluated for such Schiff bases using disc diffusion method. Molecular docking was conducted on certain penicillin-binding proteins (PBPs) and carboxypeptidases using 1- click docking software. Schiff bases of Ceftizoxime were prepared with reasonable yields and their chemical structures were confirmed by spectral analysis (FTIR, 1H-NMR) and elemental microanalysis (CHNS). The antibacter

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Publication Date
Mon Sep 11 2006
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis a nd Characterization of Some New Transition Metal Complexes of Amino Thiadiazole
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New complexes of Cu (ll), Ni (ll), Co (ll), and Zn (ll) wi th 2-amino-5-p-Fiouro Phenyl 1, 3, 4-Thiadiazole have been synthesized. The products were isolated, studied and characterized by physical measurements, ie,(Ff-IR), UV-Vis and the melting points were determined. The new Schiff base (L) has been used to prepare some complexes. The prepared complexes were identified and their structural geometry were suggested

Publication Date
Thu Jan 01 2015
Journal Name
Der Pharma Chemica
Synthesis, characterization and biological evaluation of new potentially active hydrazones of naproxen hydrazide
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To synthesize new hydrazone derivatives of naproxen with enhanced anti-inflammatory activity and devoid the ulcerogenic side effects. Hydrazones were synthesized by conjugation of naproxen hydrazide with seven natural and synthetic aldehyde and ketone by using glacial acetic acid as catalyst. The synthesis has 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.The anti- inflammatory activity of the synthesized compounds was evaluated in vivo using the egg-white induced edema model in rats, and the results of the biological assay was found to be comparable to Nap

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Publication Date
Sat Aug 30 2025
Journal Name
Iraqi Journal Of Science
Synthesis, characterization and Study of the physical properties of some new silicone polymers
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This study involves the synthesis of a new class of silicon polymers, designated as P1-P7, derived from dichlorodimethylsilane (DCDMS) in combination with various organic compounds (Schiff bases prepared from different amines and appropriate aldehydes or ketones) [I-V] through condensation polymerization. The structures of all monomers and polymers were characterization by FTIR and 1HNMR spectroscopy (for some polymers). The results of thermogravimetric analysis (TGA) and differential scanning calorimetry DSC test show stable thermal behaviour. Polymers with a higher concentration of aromatic rings in their repeating structural units exhibited a higher temperature for weight loss, indicating increased thermal stability. Thermal meas

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Publication Date
Sat Jun 01 2013
Journal Name
Journal Of The College Of Languages (jcl)
Dylan Thomas:The Vision of Death as a Prologue to a New Life
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Dylan Thomas (1914-1953) is a modern poet belongs to the apocalyptic movement of the 1940's.This movement is influenced by the doctrines and techniques of surrealism.

              Poetry for him should not be primarily concerned with man in society, but with the celebration of spiritual truth. It should bring to light the hidden causes, hence  his personal interest is to strip darkness and explore the inward motives. To do this he uses a cluster of images: a constant building up and breaking down of images. His poetry depends on the romantic spontaneity, suggestiveness of the Symbolists and the the surrealists' mysterious liberation of the unconsciousness and

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Publication Date
Sat Jun 01 2013
Journal Name
Journal Of The College Of Languages
Dylan Thomas:The vision of Death as a Prologue to a New Life
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Dylan Thomas (1914-1953) is a modern poet belongs to the apocalyptic movement of the 1940's.This movement is influenced by the doctrines and techniques of surrealism. Poetry for him should not be primarily concerned with man in society, but with the celebration of spiritual truth. It should bring to light the hidden causes, hence his personal interest is to strip darkness and explore the inward motives. To do this he uses a cluster of images: a constant building up and breaking down of images. His poetry depends on the romantic spontaneity, suggestiveness of the Symbolists and the the surrealists' mysterious liberation of the unconsciousness and the emotional involvement in the dynamics of life. In "Light Breaks

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Publication Date
Sat Jan 01 2011
Journal Name
Iraqi J Pharm Sci,
Serum Level Profile and Pharmacokinetic Parameters of Single Oral Dose of Metronidazole in Type II Diabetic Patients
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Many pathophysiological processes can affect the pharmacokinetic properties of drugs in people with diabetes. The present study was deigned to evaluate the influence of diabetes mellitus (DM) on the pharmacokinetic parameters of metronidazole administered as single oral dose. Twelve healthy volunteers and twelve diabetic patients were enrolled in the present study. On day 1, a single oral dose of metronidazole 500 mg was administered orally to all participants at 9:00 am after a 10-hour fasting. Over the following 48 hours, blood samples were taken at frequent intervals and serum metronidazole concentrations were measured by a high-performance liquid chromatography method for assessment of pharmacokinetics of metronidazole. The data

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Serum Level Profile and Pharmacokinetic Parameters of Single Oral Dose of Metronidazole in Type II Diabetic Patients
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Many pathophysiological processes can affect the pharmacokinetic properties of drugs in people with diabetes. The present study was deigned to evaluate the influence of diabetes mellitus (DM) on the pharmacokinetic parameters of metronidazole administered as single oral dose. Twelve healthy volunteers and twelve diabetic patients were enrolled in the present study. On day 1, a single oral dose of metronidazole 500 mg was administered orally to all participants at 9:00 am after a 10-hour fasting. Over the following 48 hours, blood samples were taken at frequent intervals and serum metronidazole concentrations were measured by a high-performance liquid chromatography method for assessment of pharmacokinetics of metronid

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Publication Date
Sun Mar 07 2010
Journal Name
Baghdad Science Journal
Synthesis and Polymerization of Poly Acryl Imide and One of Their Derivatives Then Curing the Product with Alkyl Halide
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The present work involved four steps: First step include reaction of acrylamide ,N-?-Methylen-bis(acryl amide) and N-tert Butyl acryl amide with poly acryloyl chloride in the presence of triethyl amine (Et3N) as catalyst, the second step include homopolymerization of all products of the first step by using benzoyl peroxide(BPO) as initiator in (80-90)Co in the presence of Nitrogen gas(N2). In the third step the poly acrylimide which prepare in second step was convert into potassium salt by using alcoholic potassium hydroxide solution. Fourth step include Alkylation of the prepared polymeric salts in third step by react it with different alkyl halides(benzyl chloride, allylbromide , methyl iodide) by using DMF as solvent for(10-12) hours.

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Publication Date
Mon Jul 01 2013
Journal Name
Journal Of Saudi Chemical Society
Synthesis, characterization and in vitro antimicrobial activity of some novel 5-substituted Schiff and Mannich base of isatin derivatives
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With the aim of developing potential antimicrobials, a series of novel Ciprofloxacin methylene isatin derivatives incorporating different aromatic aldehydes were synthesized and characterized by FTIR, 1H NMR, Mass spectroscopy and bases of elemental analysis. In addition, the in vitro antibacterial and antifungal properties were tested against some human pathogenic microorganisms by employing the disc diffusion technique. A majority of compounds were showing activity against several of the microorganisms. The relationship between the functional group variation and the biological activity of the evaluated compounds is discussed. From comparisons of the compounds, 3c was determined to be the most active compound.

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