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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
Wed Mar 25 2020
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization and Antimicrobial Evaluation of New Azo Compounds Derived from Sulfonamides and Isatin Schiff Base
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The present study deals with the synthesis of four different azo-azomethine derivatives; this is done by two steps; the first step is diazotization of sulfonamides (sulfanilamide, sulfacetamide, sulfamethoxazole, and sulfadiazine) separately, followed by the second step; the coupling reaction of diazotized compounds with isatin bis-Schiff base named 3-((4-nitrobenzylidene) hydrazono)indolin-2-one. The later one (bis-Schiff base) was synthesized by the reaction of 3-hydrazono-indolin-2-one with p-nitrobenzaldehyde. The chemical structures of newly synthesized compounds were approved on the basis of their FTIR, 1H-NMR, and CHNS elemental analysis data results. The synthesized azo compounds were tested in vitro for their antimicrobial potentia

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Publication Date
Sat Nov 04 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Preliminary Anti-Inflammatory and Anti-Microbial Evaluation of New 4,5-Dihydro-1H-Pyrazole Derivatives
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Abstract      Organic compounds with pyrazole cores have a variety of uses, notably in the pharmaceutical and agrochemical sectors. The interest in creating pyrazole compounds, examining their many features, and looking for potential uses is growing. Our work has concert with synthesis of  chalcones and pyrazolines, then finally pyrazoline-aniline derivatives and evaluation their anti-inflammatory, antibacterial and antifungal activities

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Publication Date
Tue Apr 15 2025
Journal Name
Bulletin Of The Chemical Society Of Ethiopia
Synthesis, characterization and evaluation of anticancer and antioxidant activity of new azo dye derivatives from tryptamine and complexes
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This new azo dye 3-((2-(1H-indol-3-yl) ethyl) diazenyl) quinoline-2-ol was subsequently used to prepare a series of complexes with the metal ions of Cr+3, Cu+2, VO+2, Mn+2and Mo+6. The compounds identified by 1H and 13C-NMR, FT-IR, UV-Vis, mass spectroscopy, as well as TGA, DSC, and C.H.N., conductivity, magnetic susceptibility, metal and chlorine content. The results showed that the ligand behaves in a bidantate, and that the complexes gave octahedral, excepting for VO+2 square pyramid was given, that all complexes are non-electrolytes. The effectiveness of mention the compounds in inhibiting free radicals was evaluated by the ability to act as an antioxidant was measured using DPPH as a free radical and gallic acid as a standard s

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Publication Date
Fri May 01 2015
Journal Name
Journal Of Engineering
On Gradient Descent Localization in 3-D Wireless Sensor Networks
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Localization is an essential demand in wireless sensor networks (WSNs). It relies on several types of measurements. This paper focuses on positioning in 3-D space using time-of-arrival- (TOA-) based distance measurements between the target node and a number of anchor nodes. Central localization is assumed and either RF, acoustic or UWB signals are used for distance measurements. This problem is treated by using iterative gradient descent (GD), and an iterative GD-based algorithm for localization of moving sensors in a WSN has been proposed. To localize a node in 3-D space, at least four anchors are needed. In this work, however, five anchors are used to get better accuracy. In GD localization of a moving sensor, the algo

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Publication Date
Sun Mar 15 2020
Journal Name
Iraqi Journal Of Science
Specifying Quality of a Tight Oil Reservoir through 3-D Reservoir Modeling
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Increasing hydrocarbon recovery from tight reservoirs is an essential goal of oil industry in the recent years. Building real dynamic simulation models and selecting and designing suitable development strategies for such reservoirs need basically to construct accurate structural static model construction. The uncertainties in building 3-D reservoir models are a real challenge for such micro to nano pore scale structure. Based on data from 24 wells distributed throughout the Sadi tight formation. An application of building a 3-D static model for a tight limestone oil reservoir in Iraq is presented in this study. The most common uncertainties confronted while building the model were illustrated. Such as accurate estimations of cut-off permeab

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Publication Date
Wed Dec 30 2020
Journal Name
Iraqi Journal Of Science
Specifying Quality of a Tight Oil Reservoir through 3-D Reservoir Modeling
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Increasing hydrocarbon recovery from tight reservoirs is an essential goal of oil industry in the recent years. Building real dynamic simulation models and selecting and designing suitable development strategies for such reservoirs need basically to construct accurate structural static model construction. The uncertainties in building 3-D reservoir models are a real challenge for such micro to nano pore scale structure. Based on data from 24 wells distributed throughout the Sadi tight formation. An application of building a 3-D static model for a tight limestone oil reservoir in Iraq is presented in this study. The most common uncertainties confronted while building the model were illustrated. Such as accurate estimations of cut-off

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Publication Date
Wed Sep 28 2022
Journal Name
Research Journal Of Pharmacy And Technology
Synthesis, Characterization and Preliminary Antimicrobial Evaluation of New Schiff bases and Aminothiadiazole Derivatives of N- Substituted Phthalimide
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A new series of schiff base and aminothiadiazole derivatives of N- substituted phthalimide (I-VI) were synthesized. In this work, the intermediate 4-(1,3-dioxoisoindolin-2-yl)benzaldehyde compound (I), was formed by reaction of 4-amino benzaldehyde with phthalic anhydride in glacial acetic acid(GAA). A series of Schiff bases (IV-VI) was prepared by the reaction of benzidine with compound (I) in ethanol and presence of GAA as a catalyst to form compound (IV) which react with compound (I) and p-nitro benzyldehyde to give compound (V) and (VI) respectively. A new phthalimide thiosemi-carbazone derivative (ll) was prepared by reaction of compound (l) with thiosemi-carbazide HCl in the presence of equimolar amount of sodium acetate. Fina

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Publication Date
Wed Sep 02 2020
Journal Name
International Journal Of Drug Delivery Technology
Synthesis of Levofloxacin Derivatives with some Amines and their Complexes with Copper(II) Salts and Evaluation of their Biological Activity
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Levofloxacin belongs to the fluoroquinolone family; it is a potent broad-spectrum bactericidal agent. The pharmacophore required for significant antibacterial activity is the C-3 carboxylic acid group and the 4-pyridine ring with the C-4 carbonyl group, into which binding to the DNA bases occur. In this work, we tried to show that by masking the carboxyl group through amide formation using certain amines to form levofloxacin carboxamides, an interesting activity is kept. Levofloxacin carboxamides on the C-3 group were prepared, followed by the formation of their copper complexes. The target compounds were characterized by FT-IR, elemental analysis. The antimicrobial activity of the target compounds was evaluated and showed satisfactory resu

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Publication Date
Sun Dec 25 2016
Journal Name
University Of Baghdad / College Of Education For Pure Sciences / Ibn-al-‎haitham/ Chemistry Department
Synthesis and Spectroscopic Studies and ‎Biological Activity of New Ligands ‎Containing S,N,O Donor Atoms with their ‎Metal Complexes
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The 3-aminoacetophenone and 4-aminoantipyrine were used as ‎precursors to prepare new six ligands. The three new ligands (L1,L2 ‎and L3) were synthesis by reacting one mole of 3-aminoacetophenone ‎with one mole of (Acetyl chloride), (benzoyl chloride), (4-‎methoxybenzoyl chloride) and ammonium thiocyanat in acetone as a ‎solvent, they are:-‎ L1 (AAA) =[N-(3-acetylphenylcarbamothioyl)acetamide]‎ L2 (BAA) =[N-(3-acetylphenylcarbamothioyl)benzamide]‎ L3 (MAA) =[N-(3-acetylphenylcarbamothioyl)-4-methoxy benzamide]‎ Also three new derivatives of 4-aminoantipyrine were synthesis by ‎reacting one mole of 4-aminoantipyrine with one mole of (Acetyl ‎chloride), (benzoyl chloride), (4-methoxybenzoyl chloride) and ‎ammonium thio

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Publication Date
Sun Jan 01 2017
Journal Name
Al-mustansiriyah
Synthesis, Spectroscopic and Biological Studies of a New Some Complexes with N-Pyridin-2-Ylmethyl-Benzene-1, 2Diamine
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