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Synthesis and Biological Evaluation of Two New Analogues of Gonadotropin Releasing Hormone (GnRH)D-alanine8 and D-alanine
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So far synthesis of Gonadotropin Releasing Hormone (GnRH) analogues reported in the literature has clarified some aspects of structural activity of the naturally released GnRH. As a part of continuing efforts for further understanding of this relationship, the present investigation was undertaken which involved synthesis and biological evaluation of two GnRH analogues, firstly, by replacement of the amino acid L-Argenine in the 8th position at the backbone structure of the natural hormone by the amino acid D-Alanine; and secondly, by replacement of the amino acid L-Glycine in the 10th position by D-Alanine also at the backbone structure of the nature hormone, to obtain the following analogues respectively:

PGlu-His-Trp-Ser-Tyr-Gly-Leu-DAla-Pro-Gly-NH2 (Analogue I: D-Alanine8 GnRH),

PGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-DAla-NH2 (Analogue II: D-Alanine10 GnRH), which were synthesized by applying conventional solution method. Peptides were purified by several recrystallization using appropriate solvent and proved to be homogenous. Conformity of the synthetic procedure was achieved by applying different physico-chemical analyses including Melting Point (mp), Thin Layer Chromatography (Tlc.), Infrared Spectroscopy (IR), Elemental Analysis (CHN), Amino Acid Analysis (AAA), and Nuclear Magnetic Resonance (H1NMR).Preliminary biological activity of the two analogues was determined by testing their effects of parenteral administration on ascorbic acid depletion from the ovary of pseudopregnant mice and compared with that of natural GnRH hormone. Analogue II showed significant ascorbic acid depletion as compared to the native hormone while the percentage in ascorbic acid depletion after administration of analogue I were not significant as compared to the native hormone.

Key Words: Gonadotropine releasing hormone, Peptide synthesis, Biological activity of GnRH

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Publication Date
Fri Oct 04 2024
Journal Name
Chemical Review And Letters
Newly designed 2-(aminomethyl)benzimidazole derivatives as possible tyrosine kinase inhibitors: synthesis, characterization, preliminary cytotoxic evaluation and in Silico studies
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Publication Date
Tue Aug 20 2019
Journal Name
Political Sciences Journal
"Khurasan statehood" : new centralization of ISIS and limits of incursion and development
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Abstract This study aims to discover the ways that adopted by extremism to expand to new geographical areas, in order to spread out its ideology, which led to create new geo-strategic zone, aims to recognize ISIS’s strategy to move towards new geographic locations and the motivations behind these transformations, the study also analyses all aspects of this strategy, the group’s relationship with other terrorist groups in these areas and limits of the competition between them. The study also highlights the factors that have led ISIS to move to new geographical areas and its techniques to control them.

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Publication Date
Fri Nov 01 2024
Journal Name
Current Medicinal Chemistry
Synthesis, In Silico Prediction, and In Vitro Evaluation of Anti-tumor Activities of Novel 4'-Hydroxybiphenyl-4-carboxylic Acid Derivatives as EGFR Allosteric Site Inhibitors
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Introduction:

Allosteric inhibition of EGFR tyrosine kinase (TK) is currently among the most attractive approaches for designing and developing anti-cancer drugs to avoid chemoresistance exhibited by clinically approved ATP-competitive inhibitors. The current work aimed to synthesize new biphenyl-containing derivatives that were predicted to act as EGFR TK allosteric site inhibitors based on molecular docking studies.

Methods:

A new series of 4'-hydroxybiphenyl-4-carboxylic acid derivatives, including hydrazine-1-carbothioamide (S3-S6) and 1,2,4-triazole (S7-S10) derivatives, were synthesized and characterized using IR, 1HNMR, 13CNMR

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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
THE EFFECT OF CHEMICAL AND BIOLOGICAL TREATMENTS ON IMPROVING THE NUTRITIVE VALUE OF CORN COBS AND WILD REED
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This study was conducted in Animal Resources Department , College of Agriculture to estimate the effect of chemical and biological treatments to improve the nutritive value of poor quality roughages ( corn cobs and wild reed ) . The feeds were treated chemically with 4% NaoH solution ,whereas Aspergillus niger was used to ferment corn cobs and wild reed samples . The chemical analysis showed that protein percentages of corn cobs and wild reed was increased significantly (P<0.05) from 6.05% to 10.51% and 17.70% and from 3.10 %to 6.50% and 9.96% for both chemical and biological treatments respectively. The crude fiber percentages decreased significantly (P<0.05) from 29.19% and 26.10% to 23.60% and 20.10% for chemical treatment and was 20

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Publication Date
Mon Jan 01 2024
Journal Name
Chemical Methodologies
Study of the biological activity and total antioxidant content of complexes derived from sulfonic acid and 4-hydroxybenzaldehyde
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The new liganed Schiff base named [(E)-3-hydroxy-4-((3,4,5- trimethoxybenzylidene)amino) naphthalene-1- sulfonic acid] was synthesized from 3,4,5-trimethoxybenzyldehyde and 1-amino-2-aphthol-4- sulfonic acid in equal molar ratio. A series of new metal complexes' of the common molecular formulation [M(L)2(H2O)2].H2O are synthesized and characterized by IR, UV–Vis spectra, mass spectra, atomic absorption, elemental analyses, chloride content, magnetic susceptibility and conductivity measurements as well as thermo gravimetric analysis (TGA, DSC). Consistent with results of the magnetic and spectral studies, the advised geometrical structures for all of the prepared complexes have been octahedral formula

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Publication Date
Mon Jan 01 2024
Journal Name
Heliyon
Synthesis and Characterization of Some Metal Ions Complexes with Mixed Ligand of Azo Dye and Metformin and Evaluation of its Effectiveness on the Growth of Some Pathogenic Bacteria Clinically Isolated and Study of its Toxicity on Normal and Cancerous Hepatocytes
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Publication Date
Sun Sep 01 2024
Journal Name
Heliyon
Synthesis and characterization of some Metal ions complexes with mixed ligand of azo dye and Metformin and evaluation of its effectiveness on the growth of some pathogenic bacteria clinically isolated and study of its Toxicity on normal and cancerous Hepatocytes
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Four metal compounds mixed ligand of azo dye ligand (L) and metformin.(Met) were produced at aquatic ethanol for (1:1:1) (M:L:Met). The prepared compounds were identified by utilizing atomic absorption flame, FT.IR and UV–Vis spectrum manners as well as conductivity mensuration. These compounds was assayed of the gained datum the octahedral geometry was proposed into whole prepared complexes.Also in this research was studied represented examining the antibacterial and antifungal impact of the azo dye ligand (L), metformin.(Met) and (Co,Ni, Cu and Cd complexes) on four types of pathogenic, clinically isolated bacteria that are resistant to antibiotic, like Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Klebsiella pneu

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Publication Date
Sun Sep 01 2024
Journal Name
Heliyon
Synthesis and characterization of some Metal ions complexes with mixed ligand of azo dye and Metformin and evaluation of its effectiveness on the growth of some pathogenic bacteria clinically isolated and study of its Toxicity on normal and cancerous Hepatocytes
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Publication Date
Wed Jul 01 2020
Journal Name
International Journal Of Pharmaceutical Research
Synthesis and identification of some new N-substituted quinazoline-4-one, thiazine-4-one and tetrazoline rings incorporating N-ethyl-2-(benzylthio)benzimidazole acetate and study their application as anti-oxidant agent
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Publication Date
Sun Jul 01 2018
Journal Name
Journal Of Pharmaceutical Sciences And Research
Study of Environmental and Biological characteristics of AL-Chibaish marshes and their effect to the biodiversity of southern Iraq
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The Mesopotamian marshlands faced a massive destruction from many years and this lead to effect to ecosystem. In this study a survey was made on the physical chemical and heavy metals characteristics and microbiological analysis of AL Chibaish marsh during the two months. Water analyses revealed unacceptable values for almost all physiochemical and biological properties, according to WHO standard limits for drinking water. Almost all major ions and heavy metal concentrations in water showed a distinct decreasing trend at the marsh outlet station compared to other stations. In general, major and minor ions, as well as heavy metals exhibit higher concentrations in location 1 than in location 3. The concentrations of heavy metals in water show

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