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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 Naproxen in this regard. The synthesizedhydrazone of naproxen hydrazides with their pronounced anti-inflammatory activity can enhance the anti-inflammatory activity of naproxen to a varying degree according to the type of aldehyde or ketone used.

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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of New Opioid Analgesic Peptide Analogues to Enkephalin (Leucine- and Methionine-Enkephalin)
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A small number of researches were done in the design and synthesis of enkephalin analogues that are able to resist degradation effect of proteolytic enzymes with good bioavailability and half-lives.Through studying structure activity relationships we tried to incorporate phthalyl group, tryptophan and lysine amino acids in different positions in the basic backbone structure of the naturally occurring opioid Leu5- and Met5- enkephalin, in the hope that such insertion of these amino acids could induce interesting addition in the biological activity of these analogues with enhancement of their bioavailability, in addition to decrease side effects as addiction liability.

These synthesized peptides are:

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    Publication Date
    Thu Jul 01 2021
    Journal Name
    Eurasian Chemical Communications
    Synthesis of new heterocyclic derivatives from 2-furyl methanethiol and study their applications
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    In this research, cyclic compounds derived from 2- furfural mercaptan (oxazole, triazoles) were synthesized, and their biological efficacy was measured and compared with standard drugs. Also, their effectiveness as anti-oxidant was measured and compared with ascorbic acid as a standard substance. Some of the synthesized compounds were deduced with good efficacy. © 2021 Sami Publishing Company. All rights reserved

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    Scopus
    Publication Date
    Sun Jun 09 2019
    Journal Name
    Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
    Synthesis and Preliminary Anticancer Evaluation of 6-Mercaptopurine –Methotrexate Conjugate as Possible Mutual Prodrug
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    Small molecules drug conjugate mutual prodrug design  (SMDC) composed of folate and lethal agent conjugate, rigidly bonded via hydrophilic bridge and self immolative disulfide  bond   ;  represent new interesting approaches for cancer treatment , the component of SMDC intended  for targeting    folate receptor , along with greater conservation  of component until reaching  the target tumor tissue . The  designing and synthesis of compound VI and VIII derived from 6-Mercaptopurine (6-MP) and Methotrexate ( MTX) conjugate altogether as mutual prodrugs were  processed forward  successfully by multistep reaction  procedures , and by Thin Layer Chromatography (TLC) for

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    Publication Date
    Tue Dec 01 2020
    Journal Name
    Systematic Reviews In Pharmacy
    Synthesis And Preliminary Antimicrobial Evaluation Of Schiff Bases Of N -Benzyl Isatin Derivatives
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    Isatin (1H-indole-2, 3-dione) and its analogs are an important class of heterocyclic compounds. N-benzyl isatins and Schiff bases of isatin analogs have been reported to demonstrate a variety of biological activities. This work illustrates the synthesis of new N-benzylisatin Schiff bases and studies their biological activity. Firstly, Isatin and its analogs; 5-methoxyisatin, 5-fluoroisatin reacted with benzyl iodide to obtain N-benzylated derivatives of isatins 2 (ac). Secondly, these compounds were reacted with different amines (sulphanilamide and 4-methyl sulphonyl aniline) separately, to obtain Schiff bases compounds 3 (ac) and 4 (ac), respectively. The synthesized compounds were characterized by using FT-IR and 1HNMR spectroscopy. The s

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    Publication Date
    Thu Dec 01 2022
    Journal Name
    Journal Of Chemical Health Risks
    Preparation, Characterization and Antibacterial Activity of some New Oxazolidin-5-one Derivatives Derived from Imine Compounds
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    In this research, 5- membered heterocyclic compounds as oxazolidine-5-one J1-J5 derivatives were prepared using primary aromatic amine, aromatic carbonyl compounds and chloroacetic acid. By combining primary aromatic amines and aromatic carbonyl compounds, Schiff's bases were synthesized. Schiff bases are used with the chloroacetic acid compound to prepare oxazolidine-5-one J1-J5 derivatives. The compounds J1-J5 were described using NMR spectroscopy and FT-IR. .The biological efficacy was evaluated according to maximum inhibitory concentrations (MICs) toward Staphyloccoccus aureus and Esherichia coli. The best MIC was 210 μg ml-1 for J4 against the two pathogenic bacteria, while J1, J4, and J1 did not show any inhibitory effect against all

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    Publication Date
    Wed Oct 04 2023
    Journal Name
    History Of Medicine
    Theoretical Biological Activities and Docking studies of new amino-acids Derivatives of Oseltamivir for The Treatment of Coronavirus Disease 2019
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    Antiviral medications may be the best choices for COVID-19 treatment until particular therapeutic treatments become available. Tamiflu (oseltamivir) is a neuraminidase inhibitor licensed for the management and defense against influenza types A and B. Oseltamivir-based medication combinations are currently being used to treat COVID-19 patients who also have the new coronavirus 1 SARS-CoV-2. 1 Oseltamivir administration was related with a less time spent in the hospital, quicker recovery 1 and discharge, and a decreased mortality rate. Docking is a modern computational method for identifying a hit molecule by assessing the binding ability of molecular medicines within the binding target pocket. In this work, we chose 21 ligand compounds that

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    Publication Date
    Thu Dec 01 2011
    Journal Name
    Journal Of Economics And Administrative Sciences
    Dynamic algorithm (DRBLTS) and potentially weighted (WBP) to estimate hippocampal regression parameters using a techniqueBootstrap (comparative study)
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    Bootstrap is one of an important re-sampling technique which has given the attention of  researches recently. The presence of outliers in the original data set may cause serious problem to the classical bootstrap when the percentage of outliers are higher than the original one. Many methods are proposed to overcome this problem such  Dynamic Robust Bootstrap for LTS (DRBLTS) and Weighted Bootstrap with Probability (WBP). This paper try to show the accuracy of parameters estimation by comparison the results of both methods. The bias , MSE and RMSE are considered. The criterion of the accuracy is based on the RMSE value since the method that provide us RMSE value smaller than other is con

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    Publication Date
    Tue Jul 09 2019
    Journal Name
    Journal Of Global Pharma Technology
    Ni (II) and Cd (II) Complexes Derivatives from Heterocyclic Schiff Base; Synthesis, Spectroscopic and Biological Studies
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    Ni and Cd complexes of new Schiff base derived from 5-Amino-2-phenyl-2,4-dihydro-pyrazol-3-one with 4-chlorobenzalaldehyde (A) , 2-Hydroxy-benzalaldehyde (B) and 4-Hydroxy-benzaldehyde (C) have been prepared and characterized by elemental analysis , molar conductivity measurements , FTIR , UV- vis , 1HNMR, mass spectrometer and magnetic susceptibility. Analytical data revealed that six complexes were a distorted tetrahedral geometry and exhibited (1:1) metal :ligand ratio. The biological activity for the three ligands and its complexes were studied

    Publication Date
    Thu Jul 01 2004
    Journal Name
    Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
    NEW RECORD OF SOME BIOLOGICAL ENEMIES OF CITRUS LEAFMINER Phyllocnistis citrella Stainton (Lepidoptera: Gracillaridae) IN IRAQ
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    An extensive survey of citrus leaf miner (CLM) , Phyllocnistis citrella Stainton parasites
    and predators was conducted during 1998 and 1999 in citrus orchards and nursuries in
    Baghdad, Diyala and Wasit .Five eulophid parasites were recorded for the first time on citrus
    leaf miner larvae , prepupae and pupae viz. Cirrospilus sp, Pnigalio sp ., Ratzburgiola
    incompleta , Tetrasticus sp. and, Neochrysocharis formosa . Parasitism rate was ranged from
    15% to 63% Chrysopa carnea , Orius albidipennis , Amblyseius sp . Were observed as
    predators on CLM .

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    Publication Date
    Wed Nov 05 2014
    Journal Name
    International Journal Of Applied Mathematical Research
    Approximate solution of a model describing biological species living together using a new iterative method
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