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Design and Synthesis of Novel Derivatives of 4-(6-(4-Substituted Phenyl)-7H-[1,2,4] Triazolo[3,4-b][1,3,4]Thiadiazin-3- yl) Phenol as a Potent Inhibitor of Tubulin with Antitumor Activity
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Publication Date
Sun Dec 04 2016
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New 2-Quinolone Sulfonamide Derivatives
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A series of new 2-quinolone derivatives linked to benzene sulphonyl moieties were performed by many steps: the first step involved preparation of different coumarins (A1,A2) by condensation of different substituted phenols with ethyl acetoacetate. The compound A1 was treated with nitric acid to afford two isomers of nitrocoumarin derivatives (A3) and (A4). The prepared compounds (A2, A3) were treated with hydrazine hydrate to synthesize different 2-quinolone compounds (A5,A6) while the coumarin treated with different amines gave compounds (A7,A8). Then the synthesized 2-quinolone compounds (A5-A8) treated with benzene sulphonyl chloride to afford new sulfonamide derivatives (A9-A12). The synthesized compounds were characterized by FT-IR, 1H

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Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization, and Antimicrobial Evaluation of New Ceftriaxone Derivatives
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The present study was designed to synthesize a number of new Ceftriaxone derivatives by its involvement with a series of different amines, through the chemical derivatization of its 2-aminothiazolyl- group into an amide with chloroacetyl chloride, which on further conjugation with these selected amines will produce compounds with pharmacological effects that may extend the antimicrobial activity of the parent compound depending on the nature of these moieties.

Ceftriaxone was first equipped with a spacer arm (linker) by the action of chloroacetyl chloride in aqueous medium and then further reacted with seven different aliphatic and aromatic amines which resulted in the production of the aimed final target products. The syntheses

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Publication Date
Sat Jun 19 2021
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Antibacterial Evaluation of Some Coumarin Derivatives
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Coumarin derivatives have shown different biological activities, such as antifungal, antibacterial   antiinflammatory, and antioxidant activities, besides antibiotic resistance modulating effects, and anti-HIV, hepatoprotective, and antitumor effect. So, new coumarin derivatives (hydrazones and an amide) were synthesized through multisteps reactions. All the synthesized target compounds were characterized by FT-IR spectroscopy, 1HNMR analysis. The compounds then evaluated for their anti-bacterial activity by means of well-diffusion method against two gram-positive bacteria (Staphylococcus aureus, Streptococcus pneumoniae) and two gram-negative bacteria  (E.coli and Pseudomonas aeruginosa). The highest activity was demonstr

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Publication Date
Thu Feb 01 2024
Journal Name
Surface Engineering And Applied Electrochemistry
Synthesis of New 1,2,4-Triazole Containing Copolymers and Their Corrosion Inhibition оf Mild Steel in Acidic Medium
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Publication Date
Sat Feb 01 2025
Journal Name
Advanced Journal Of Chemistry, Section A
Synthesis and Characterization of Heterocyclic Derivatives to Evaluate their Efficiency as Corrosion Inhibitors for Carbon Steel in Saline Medium
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This work includes preparation of Az, Qz, and Tz derivatives from the reaction of Schiff base (Sb) derivative with anthranilic acid, chloroacetyl chloride, and sodium azide, as well as, the characterization via FT-IR, 1H-NMR, and 13CNMR. The anticorrosion inhibition of these compounds was studied and the measurements of carbon steel (CS) corrosion in sodium chloride solution 3.5% (blank) and inhibitor in solutions were calculated at a temperature range of 293-323 K by the technique of electrochemical polarization. In addition, some thermodynamic and kinetic activation parameters for inhibitor and blank solutions (Ea⋇, ΔH⋇, ΔS⋇, and ΔG⋇) were determined. The results showed high inhibition efficacy for all the prepared compounds,

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Publication Date
Tue Sep 02 2025
Journal Name
Chemistry & Biodiversity
Synthesis, In Silico, and Biological Evaluation of Non‐Hydroxamate Benzoic Acid–Based Derivatives as Potential Histone Deacetylase Inhibitors (HDACi)
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ABSTRACT<p>Unregulated epigenetic modifications, including histone acetylation/deacetylation mediated by histone acetyltransferases (HATs) and histone deacetylases (HDACs), contribute to cancer progression. HDACs, often overexpressed in cancer, downregulate tumor suppressor genes, making them crucial targets for treatment. This work aimed to develop non‐hydroxamate benzoic acid–based HDAC inhibitors (HDACi) with comparable effect to the currently four FDA‐approved HDACi, which are known for their poor solubility, poor distribution, and significant side effects. All compounds were structurally verified using FTIR, <sup>1</sup>HNMR, <sup>13</sup>CNMR, and mass spectrometry. In silico ana</p> ... Show More
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Publication Date
Fri Jun 01 2018
Journal Name
Journal Of Global Pharma Technology
Synthesis, Spectral Studies and Biological Activity of Azo dye Complexes with Some MetalIons
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2-(2-amino-5-nitro-phenylazo) -phenol was ready by grouping the diazonium salt of 2-aminophenol with 4-nitroaniline.Thegeometry of azo ligand(HL)was resolved on the origin of (C.H.N) analysis, 1H and 13CNMR spectra, infrared spectra and UV–vis electronic absorption spectra. Dealing with the azo ligand produced with Nd+3,Cd+3,Dy+3 and Er+3at aqueous ethanol for a 1:2 metal: ligand rate, and in perfect ph. The formation for compounds have been described by utilizing flame atomic absorption,(C.H.N) Analyses, conductivity, infrared spectra and UV–vis spectral procedures. Nature in the produced compounds have been studied obey the ratio of mole and continuous variance manners, Beer's law yielded up a concentration rate (1×10-4 - 3×10-4M) .

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Publication Date
Tue Jul 10 2018
Journal Name
Journal Of Global Pharma Technology
Synthesis, Spectral Studies and Biological Activity of Azo dye Complexes with Some MetalIons
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2-(2-amino-5-nitro-phenylazo),-phenol was ready by grouping the diazonium salt of 2-aminophenol with 4-nitroaniline.Thegeometry of azo ligand(HL)was resolved on the origin of (C.H.N) analysis,1H and 13CNMR spectra, infrared spectra and UV–vis electronic absorption spectra. Dealing with the azo ligand produced with Rh+3 and La+3ataqueous ethanol for a 1:3 metal: ligand rate, and in perfect ph. The formation for compounds have been described by utilizing flame atomic, absorption,(C.H.N),Analyses, conductivity, infrared spectra and UV–vis spectral procedures. Nature in the produced compounds, have been studied, obey the ratio of mole and continuous, variance, manners, Beer's law, yielded up a concentration, rate (1×10-4- 3×10-4M),. High

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Publication Date
Sat Jun 29 2024
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Characterization of New 5-Fluoroisatin-Chalcone Conjugates with Expected Antimicrobial Activity
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Pathogenic microorganisms are becoming more and more resistant to antimicrobial agents. So the synthesis of new antimicrobial agents is very important. In this work, new 5-fluoroisatin-chalcone conjugates 5(a–g) were synthesized based on previous research that showed the modifications of the isatin moiety led to the synthesis of many derivatives that have antimicrobial activity. 4-aminoacetophenone reacts with 5-fluoroisatin to form Schiff base (3), which in turn reacts with two different groups of aromatic (carbocyclic and heterocyclic) aldehydes 4(a–g) separately to form the final compounds 5(a–g). Proton-nuclear magnetic resonance (¹H-NMR) and Fourier-transform infrared (FT-IR) spectroscopy were used to confirm the chemic

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Publication Date
Mon Jan 01 2018
Journal Name
Journal Of Pharmacy Research
Design and in vitro characterization of bisacodyl as a hollow-type suppositories
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