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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
Sat Jan 01 2022
Journal Name
Egyptian Journal Of Chemistry
Structural, Characterization and Biological Activity of New Ligand N-(Pyrimidin-2-Yl Carbamothioyl) Acetamide and Its Complexes With (VO(II), Mn (II), Cu (II), Zn (II), Cd (II) and Hg (II)
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New ligand of N-(pyrimidin-2-yl carbamothioyl)acetamide was synthesized and its complexes with (VO(II), Mn (II), Cu (II), Zn (II), Cd (II) and Hg (II) are formed with confirmation of their structures on the bases of spectroscopic analyses. Antimicrobial activity of new complexes are studied against Gram positive S. aureus and Gram negative E. coli, Proteus, Pseudomonas. The octahedral geometrical structures are proved depending on the outcomes from the preceding procedures. Keywords: pyrimidin-2-amine, acetyl isothiocyanate, complexes, Antimicrobial activity

Publication Date
Thu Jan 01 2009
Journal Name
مجلة ديالى للبحوث الانسانية
Synthesis and study of new Macrocyclic ligand type N2O2 and its complexes with (Co (II) ,Ni (II) ,Cu (II) ,Zn (II) and Cd (II)) ions.
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A new Schiff base ligand [L] [3-methyl-9,10 phenyl -6,7 dihydro-5,8 –dioxo-1,2 diazo –cyclo dodecu 2,11-diene ,4-one ] and its complexes with (Co(II), Ni(II), Cu (II), Zn(II) and Cd(II)) were synthesis.This ligand was prepared in three steps, in the first step a solution of salicyladehyed in methanol reacted under refluxed with hydrazine monohydrate to give an (intermediate compound 1) which reacted in the second step with sodium pyruvate to give an (intermediate compound 2) which gave the ligand [L] in the three step when it reacted with 1,2- dichloro ethane.The complexes were synthesized by direct reaction of the corresponding metal chloride with the ligand. The ligand and complexes were characterized by spectroscopic methods [IR, UV-

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Publication Date
Mon Sep 11 2006
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis a nd Characterization of Some New Transition Metal Complexes of Amino Thiadiazole
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New complexes of Cu (ll), Ni (ll), Co (ll), and Zn (ll) wi th 2-amino-5-p-Fiouro Phenyl 1, 3, 4-Thiadiazole have been synthesized. The products were isolated, studied and characterized by physical measurements, ie,(Ff-IR), UV-Vis and the melting points were determined. The new Schiff base (L) has been used to prepare some complexes. The prepared complexes were identified and their structural geometry were suggested

Publication Date
Wed Aug 28 2019
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization and Screening their Antibactrial Activity of some New Oxazepine and Diazepine Compounds Containing 1,3,4-Oxadiazole Ring Derived from L-Ascorbic Acid
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The search involve the synthesis of some new 1,3-oxazepine and 1,3-diazepine derivatives were synthesized from Schiff base. The Schiff base (VIII) prepared from reaction of aldehyde (IV) derived from L-ascorbic acid with aromatic amine ([2-(4- nitrophenyl)-5-(4-aminophenyl)-1,3,4-oxadiazole] (VII). Oxazepine compounds (IX-XI) were synthesized from the cyclic condensation of Schiff base (VIII) with (maleic, phthalic and 3-nitrophthalic) anhydride, compounds (IX-XI) that were reacted with p-methoxyaniline to give diazepine derivatives (XII-XIV). The structures of the new synthesized compounds have been confirmed by physical properties and spectroscopy measurements such as FTIR, and some of them by 1 H-NMR, 13 CNMR, Mass, and evaluated

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Publication Date
Thu Jan 02 2014
Journal Name
Journal Of The Faculty Of Medicine Baghdad
Serum parathyroid hormone and total serum calcium levels in mild & severe preeclampsia versus normal pregnancy
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Background: Preeclampsia (PE) is a major cause of maternal morbidity and mortality, complicating 3-14% of all pregnancies. Although the etiology remains unknown, placental hypoperfusion and diffuse endothelial cell injury are considered to be the central pathological process; many endocrinological changes have been linked to the etiology of preeclampsia including parathyroid hormone and calcium level. Objective: to compare serum parathyroid hormone and total serum calcium levels in mild and severe preeclampsia versus normal pregnancy. Patients and methods: Serum parathyroid hormone (PTH) level and total serum calcium level were measured in thirty normotensive pregnant women and thirty women with mild preeclampsia and thi

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Publication Date
Mon Dec 05 2022
Journal Name
Baghdad Science Journal
Synthesis, Identification, Theoretical Study, and Effect of the New Heterocyclic System from Ciprofloxacin Derivatives on the Activity of Some Liver Enzymes
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The target of this study was to synthesize several new Ciprofloxacin drug analogs by providing a nucleophilic substitution procedure that provides new functionality at the carboxylic group location. The analogs were synthesized, designed, and characterized by 1HNMR, and FTIR. The synthetic path began from the reaction of ciprofloxacin drug with morpholine to give compound[B], ciprofloxacin derivative was linked with a variety of primary and secondary amines to give compounds[B1-B9]. The above-mentioned prepared compounds [B3 and B5] were applied to liver enzymes, and the increase in the activity of these enzymes was observed. In addition, a theoretical study was conducted to study the energies and properties of the prepared co

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Publication Date
Mon Nov 18 2024
Journal Name
Molecular Crystals And Liquid Crystals
Synthesis and liquid crystal properties of a new class of calamitic mesogens based on twin 1,3,4-thiadiazole derivatives with imine linkage
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Publication Date
Sun Mar 01 2015
Journal Name
Journal Of The Chilean Chemical Society
NEW AZO-SCHIFF BASE DERIVED WITH Ni(II), Co(II), Cu(II), Pd(II) AND Pt(II) COMPLEXES: PREPARATION, SPECTROSCOPIC INVESTIGATION, STRUCTURAL STUDIES AND BIOLOGICAL ACTIVITY
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The coordination ability of the azo-Schiff base 2-[1,5-Dimethyl-3-[2-(5-methyl-1H-indol-3-yl)-ethyl imino]-2-phenyl-2,3-dihydro-1H-pyrazol-4-ylazo]-5- hydroxy-benzoic acid has been proven in complexation reactions with Co(II), Ni(II), Cu(II), Pd(II) and Pt(II) ions. The free ligand (LH) and its complexes were characterized using elemental analysis, determination of metal concentration, magnetic susceptibility, molar conductivity, FTIR, Uv-Vis, (1H, 13C) NMR spectra, mass spectra and thermal analysis (TGA). The results confirmed the coordination of the ligand through the nitrogen of the azomethine, Azo group (Azo) and the carboxylate ion with the metal ions. The activation thermodynamic parameters, such as ΔE*, ΔH*, ΔS*, ΔG*and K are cal

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Publication Date
Thu Feb 02 2012
Journal Name
Wasit Journal For Science And Medicine
Field study for the effect of releasing predator Chrysoperla carnea (Stephens) (Neuroptera:Chrysopidae) in comparison with Deltamethrin in controlling cabbage aphid
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Publication Date
Sun Jun 25 2023
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization, Antioxidant and Antibacterial Studies for New Schiff Base Complexes derived from 4-Bromo-O-toluidine
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In this article, new Schiff base ligand LH-prepared Mn(II), Co(II), Ni(II), Cu(II), Zn(II), Cd(II), Hg(II), Pd(II), and Pt(II) materials were analyzed using spectroscopy (1 Metal: 2 LH). The ligand was identified using techniques such as FTIR, UV-vis, 1H-13C-NMR, and mass spectra, and their complexes were identified using CHN microanalysis, UV-vis and FTIR spectral studies, atomic absorption, chloride content, molar conductivity measurements, and magnetic susceptibility. According to the measurements, the ligand was bound to the divalent metal ions as a bidentate through oxygen and nitrogen atoms. The complexes that were created had microbicide activity against two different bacterial species and one type of fungus. DPPH techniques were bei

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