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Synthesis of new Conjugates of some NSAIDs with Sulfonamide as Possible Mutual Prodrugs using Tyrosine Spacer for Colon Targeted Drug Delivery
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The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of  inflammation and infections in colon).

Key words: Mutual prodrug, Ester linkage, Azo bond, Colon targeting

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Publication Date
Sun Dec 30 2018
Journal Name
Baghdad Science Journal
Synthesis and study of biological activity of some new Imidazole derivatives
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In this work ester derivatives were synthesized by the reaction of imidazole derivatives (C1) with ethylchloroacetate in ethanol and NaOH to give the corresponding (C2) .While compound (C3) acetohydrazide was synthesized by the reaction of ester derivatives (C2) with hydrazine hydrat in ethanol. Compound (C3) from the reaction with different aromatic aldehydes in absolute ethanol gave the Schiff′s bases (C4,C5). The product compounds were characterized by FT-IR, U.V and 1HNMR spectra and the biological activities were studied as antibacterial.

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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 some Novel Nitrogenous Heterocyclic Compounds with Expected Biological Activity as Antimicrobial and Cytotoxic Agents
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This study includes synthesis of some nitrogenous heterocyclic compounds linked to amino acid esters or heterocyclic amines that may have a potential  activity as antimicrobial and/or cytotoxic.  Quinolines are an important group of organic compounds that possess useful biological activity as antibacterial, antifungal and antitumor .8-Hydroxyquinoline (8-HQ) and numerous of its derivatives exhibit potent activities against fungi and bacteria which make them good candidates for the treatment of many parasitic and microbial infection diseases.

These pharmacological properties of quinolones  aroused our  interest in synthesizing several new compounds featuring heterocyclic rings of the quinoline derivatives linke

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Publication Date
Fri Jan 20 2023
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis, Spectroscopic, and Biological Activity Study for New Complexes of Some Metal Ions with Schiff Bases Derived From 2-Hydroxy Naphthaldehyde with 2-amine benzhydrazide
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This study describes the preparation of tetradentate Schiff base derived from the condensation of 2-Hydroxy naphthaldehyde with 2-amine benzhydrazide and the synthesis of new complexes series with a good yield.The prepared ligand was characterized using a microanalysis technique, UV-visible, FT-IR, nuclear magnetic resonance 1H-NMR, mass spectrometry, thermal gravimetric analysis TGA, and the addition of conductivity measurement and magnetic moment of complexes. The invitro antimicrobial activity of the prepared compounds was tested against  Gram-negative Klebsiella pneumonia, Gram-positive Staphylococcus aureu, and Candida albicans by the agar well diffusion method. The spectroscopy and measurement studies showed that the li

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Publication Date
Fri Jan 26 2024
Journal Name
Iraqi Journal Of Science
Quantum Mechanical Calculations of R-O Thermal Bond Rupture Energies in Some Ampicillin Prodrugs
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PM3 and Unrestricted Hartree Fock (UHF) quantum mechanical methods are carried out for the estimation of reaction path for the breakage of (R-O) bond rupture energies, for twelve ampicillin ester prodrugs derivatives, at their calculated equilibrium geometries, in addition to some physical properties such as heat of formation, total energy, dipole moment and the energy difference of EHOMO and ELUMO (ΔEHOMO-LUMO) energy levels, using the Gaussian-03 program. Comparisons were done between the total energies of the reactants, products, activation energies and transition states. The results show non possible use of some substituted organic groups as a carrier linkage for acidic ampicillin drug, whereas others show possible use as a carrier

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Publication Date
Sun Oct 15 2023
Journal Name
Journal Of Yarmouk
Artificial Intelligence Techniques for Colon Cancer Detection: A Review
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Publication Date
Fri Dec 08 2023
Journal Name
Iraqi Journal Of Science
Synthesis, Characterization and Evaluation of Some Pyranopyrazoles and Pyranopyrimidines Derivatives as Antioxidants for Lubricating Oils
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6-Amino-4-(4-hydroxyphenyl)-5-cyano-3-methyl-1-phenyl-1, 4-dihydropyrano [2,3-c] pyrazole (compound 2) was prepared by condensation of 2-(4-hydroxylbenzylidine) malononitrile (compound 1) [which was prepared by Knoevenagel condensation of malononitrile with 4-hydroxy benzaldehyde ] with 3-methyl-1-phenyl-2-pyrazolin-5-one. Reactions of compound 2 with different reagents formic acid, formamide, and ammonium thiocyanate under microwave irradiation leads to the synthesis of 4-(4-hydroxyphenyl)- 3-methyl-1-phenyl-4,6-dihydro- pyrazolo [3', 4':5,6] pyrano [2,3-d] pyrimidine-5-one (compound 3), 4-(4-hydroxyphenyl)- 3-methyl-1-phenyl-4, 6-dihydro- pyrazolo [3', 4':5,6]pyrano[2,3-d]pyrimidine-5-imine (compound 4) and N-[4-(4-hydroxyphenyl)- 3-me

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Publication Date
Sun Jul 31 2022
Journal Name
Iraqi Journal Of Science
Synthesis, Characterization and Evaluation of Some Pyranopyrazole Derivatives as Multifunction Additives for Medium Lubricating Oils
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      The current work involves synthesis of 6-amino-4-(4-hydroxyl-3-methoxyphenyl)-3-methyl-1-phenyl-1,4- dihydropyrano[2,3-c]pyrazole-5-carbonitrile (2) by condensation of 2-(4-hydroxyl-3-methoxybenzylidine) malononitrile (1) with 3-methyl-1-phenyl-2-pyrazolin-5-one. The product 2 was then reacted with various aldehydes to form a series of Schiff base derivatives 3a-h. The reaction of the chosen Schiff base derivatives (3a and 3b) with mercaptoacetic acid gave thiazolidinone derivatives (4a and 4b). The structures of prepared compounds were confirmed using FT-IR, 1H NMR, and 13

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Publication Date
Sun Apr 30 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis, Spectroscopic and Biological Studies of a New Some Complexes with N-Pyridin-2-Ylmethyl-Benzene-1,2Diamine
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 N-Pyridin-2-ylmethyl-benzene-1,2-diamine (L) was prepared from the reaction of ortho amino phenyl thiol with 2 – amino methyl pyridine in mole ratio (1:1) . It was characterized by elemental analysis (C.H.N) , FT-IR , Uv – Vis , 1H , 13C-N.M.R . The complexes of the bivalent ions (Co , Ni , Cu ,Pd , Cd , Hg and Pb) and the trivalent (Cr) have been prepared and characterized too . The structural was established by elemental analysis (C.H.N) , FT-IR , Uv – Vis spectra , conductivity measurements , atomic absorption and magnetic susceptibility . The complexes showed characteristic behavior of octahedral geometry around the metal ions and the (N,N,N) ligand coordinated in tridentat mode except with Pd complexes sho

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Publication Date
Sat Dec 30 2023
Journal Name
Iraqi Journal Of Science
Synthesis and Structural Views on New Azo Ligand and Its Metal Complexes with Some of their Application
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     In this work,  we presented a study of the structural formula for a new series of complexes with Ag(I), Cu(II), Zn(II), and Cd(II) derived from the guanine azo dye ligand 2-amino-8-((3-hydroxyphenyl)diazinyl)-1,7-dihydro-6H-purin-6-one (HAG), which is investigated using various physicochemical analyses, spectroscopic techniques (FT-IR, U.V-VIS, and 1H NMR), thermogravimetric analysis (TGA). In addition, elemental analyses, magnetic susceptibility, and molar conductance measurements were all stabilized. As well as the mole ratio, stability constant, and Gibbs free energy were studied for all complexes, where they showed high stability and spontaneous synthesis. The Cu(II) complex was suggested to have octahedral stere

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Publication Date
Fri Sep 02 2022
Journal Name
Military Medical Science Letters
SOLID LIPID NANOPARTICLES AS A PROMISING APPROACH FOR DELIVERY OF ANTICANCER AGENTS: REVIEW ARTICLE
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Cancer disease has a complicated pathophysiology and is one of the major causes of death and morbidity. Classical cancer therapies include chemotherapy, radiation therapy, and immunotherapy. A typical treatment is chemotherapy, which delivers cytotoxic medications to patients to suppress the uncontrolled growth of cancerous cells. Conventional oral medication has a number of drawbacks, including a lack of selectivity, cytotoxicity, and multi-drug resistance, all of which offer significant obstacles to effective cancer treatment. Multidrug resistance (MDR) remains a major challenge for effective cancer chemotherapeutic interventions. The advent of nanotechnology approach has developed the field of tumor diagnosis and treatment. Cancer nanote

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