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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
Sun Dec 20 2020
Journal Name
International Journal Of Pharmaceutical Research
Synthesis, Characterization and Biological Activity of New Compounds Derived from Dapsone
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New derivatives of the anti-inflammatory, leprostatic drug dapsone 4 are synthesized, characterized and biologically screened by the treating the drug dapsone with chloroacetyl chloride in the presence of base. Both amino groups are acylated to give compound 6. The symmetrical acylated product then treated with Phenol, N-Acetyl-p-aminophenol, p-Chlorophenol, m-Chlorophenol, o-Hydroxybezoic acid and m-Hydroxybezoic acid to give compounds 8(a-f). The antimicrobial activity was tested for the synthesized compounds; activates were good compared to the parent drug. All the new compounds have scanned for their biological activities toward gram ‒ve and gram +ve (M. tuberculosis, S. pneumoniae, E. coli and P. mirabilis) bacteria, the synthesized

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Publication Date
Fri Apr 01 2022
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New Benzothiazole-derived Schiff Bases Metal Complexes
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Nitrogen-comprising heterocyclic compounds and their derivatives have empirically been invaluable as therapeutic agents. Fundamentally, 4-chloro-6-nitro-2-amino-1,3-benzothiazole 1 was synthesized via bromination of 2-chloro-4-nitro aniline with ammonium thiocyanate. This new heterocyclic haloorganoamino-1,3-benzothiazole derivative, was a starting material, which condensed and tethered with three different aromatic aldehyde pendant arm in presence of ethanol and glacial acetic acid isolating an interesting sequence of tridentate Schiff bases 2-4. These compounds were used for complexation reactions in 1:1 (metal: ligand) stoichiometry to obtain heteroleptic Al(III), Ni (II) and K(I) benzothiazole chelat

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Publication Date
Tue Sep 23 2025
Journal Name
Arabian Journal For Science And Engineering
Shear Thickening Behaviour of Cross-Linked Polyacrylamide Gels Induced by Gas Flow in Porous Media
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Excessive water production is a persistent challenge in oil and gas wells, with polymer and gel solutions commonly employed for water control. This study investigates the rheological behaviour of cross-linked polyacrylamide gels and their impact on water shutoff treatment in gas wells. Rheological measurements, coreflooding experiments using Berea sandstone samples, and micromodel flow visualizations were conducted to evaluate gel performance. Results showed that during water injection, the water residual resistance factor ( Frrw ) decreases with increasing flow rates, mainly due to gel shear thinning behaviour and reduced residual gas saturation. Higher polymer concentrations in the gel enhance water permeability reduction. In contrast, un

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Publication Date
Thu Jul 01 2021
Journal Name
International Journal Of Drug Delivery Technology
Synthesis and Diagnosis of Some Derivatives of 1,2,4-Triazole-3-Dicarboxylic Acid and Study their Biological Activity
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Newly prepared derivatives of Heterocyclic of dicarboxylic acid include 1, 2, 4-Triazoledicarboxylic acid. Thiocarbohydrazine (TCH) reacts with aliphatic and aromatic dicarboxylic acids, and when these resulting compounds interact with compounds containing a group of carbonyl they result in Schiff base, which are very important in the industrial and medical fields and the acids used (oxalic acid, succinic, terephthalic) to prepare the triazole, then the reaction with Para-chlorobenzendihaide. and some physical properties were measured for these products. The biological activity of the prepared compounds has been studied, and it has been shown that they have different effects on the bacteria, compounds prepared with Fourier Transform Infrare

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Publication Date
Mon Aug 08 2022
Journal Name
Egyptian Journal Of Chemistry
Synthesis, spectroscopic and liquid crystalline studies of dithiocarbamat derivatives of pyrazole type ligands and their metal complexes
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Publication Date
Mon Jun 25 2018
Journal Name
Oriental Journal Of Chemistry
Advancement and Validation of new Derivatives Spectrophotometric Method for Individual and Simultaneous Estimation of Diclofenac Sodium and Nicotinamide
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Publication Date
Mon Mar 27 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
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 (1

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Publication Date
Fri Jan 19 2018
Journal Name
Journal Of Global Pharma Technology
Synthesis, Characterization and Study of Electrical Properties of Some New Aromatic Polyester
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This research discloses the synthesis of various polyester resins, the polyesters containing homoring aromatic and others heterocyclic were synthesized by the condensation polymerization of suitable monomers (which are containing variety function groups in different structures) with phthalic anhydride. The main objective is synthesis of new polyester with keeping a reasonable electrical insulating behavior. The structural of polymer was characterized by Fourier Transform infra-red spectroscopy FTIR and HNMR. The dielectric constant (real ε' and imaginary parts ε") and AC conductivity (σAC) for all the polyester samples are studied by varying the frequency (30, 50, 70, 90, 120, 300, 500Hz and 1KHZ) at 25⁰ C. Indeed, study of the electri

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Publication Date
Wed Apr 30 2025
Journal Name
Academic Science Journal
Synthesis, Characterization and Study of Biological Activity of Some New Schiff Bases
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            In the present study, ( Schiff's bases 6a - 6e) and  (new amids derivatives 6f - 6j) have been synthesized . The glutaroyl chloride(2) has been prepared by the reacting of glutaric acid and thionyl chloride in presence of (DMF) . The new compound bis(4-formylphenyl) glutarate (3) has been Synthesized from reaction of one mole of glutaroyl chloride and two moles of 4-hydroxybenzaldehyde . Compound 4,4'-(glutaroylbis(oxy))dibenzoic acid (4) was Synthesized from one mole of glutaroyl chloride and two moles of 4-hydroxybenzoic acid, while compound bis(4-(chlorocarbonyl)phenyl) glutarate (5) was prepared from 4,4'-(glutaroylbis(oxy))dibenzoic acid and Thionyl chloride . Then Schiff's bases 6a - 6e that prepared

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Publication Date
Sun Mar 03 2013
Journal Name
Baghdad Science Journal
Synthesis and Identification of Some New Derivative of Trimethoprim and Paracetemol Drugs
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In this research two series of the new derivatives of Trimethoprim and paracetamol drugs have been prepared which known as a high medicinal effectiveness. Series (A) is including the interaction of diazonium salt of trimethoprim and coupling with some substituted phenol compounds (2-amino phenol, 3-ethyl phenol, 1-naphthol, 2-nitro phenol, Salbutamol). Series (B) is including the interaction coupling alkali solution of paracetamol with diazonium salt of some substituted aniline compounds (Benzedine, 2, 3-di chloro aniline, Trimethoprim, Anilinium chloride, 2-nitro- 4-chloro aniline).Chemical structures of all synthesized compounds were confirmed by UV-visible and FTIR spectroscopy.

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