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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:

  • Analogue I: phthalyl-tyrosyl-glycel-tryptophan methyl ester.
  • Analogue II: Boc-tyrosyl-glycyl-phenylalanyl-lysine ethyl ester. HBr.

According to the designed structures, the analogues were synthesized following the conventional solution method and they were identified using the following techniques: melting point, optical rotation, thin layer chromatography (TLC), infrared spectroscopy (IR), elemental analysis (CHN) and amino acid analysis.

Key words: peptide, phthalyl, opoioid analgesics

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Publication Date
Mon Mar 15 2021
Journal Name
Egyptian Journal Of Chemistry
Antimicrobial Activity of New Synthesized Aza -Beta Lactam and Tetrazole Derivatives Bearing Imidazo[2,1-B]Benzothiazole Moiety
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Publication Date
Sun Sep 04 2016
Journal Name
Baghdad Science Journal
Synthesizing, Characterizing and Studying the Biological Activity of Some New Schiff-Bases Derivatives Containing the Monosaccharide Moiety
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A new series of ?-D-glucose as Schiff bases derivatives is synthesized and characterized with studying their bioactivity. Hydroxyl groups at C (1,2&5,6) sugar moiety are converted into acetal form through a reaction with dry acetone using phosphoric acid and anhydrous zinc chloride as catalysts producing 1,2:5,6-di-O-isopropyledine ?-D-glucofuranose(I). The five memberd ring acetal of C(5,6) is hydrolyzed with acetic acid (65%)and a reaction of the new product with sodium periodate is carried on to get an aldehyde moiety which is used to produce a new series of Schiff bases through reacting with different amino compounds such as 4-amino antipyrene . The suggested chemical structures of the prepared compounds are confirmed by using UV., FT

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Publication Date
Tue Jul 17 2018
Journal Name
Journal Of Global Pharma Technology
Preparation, Characterization and Biological Activity Studies of Some Metal Complexes with New Schiff Base for Trimethoprim Ligand
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A new ligand complexes have been synthesis from reaction of metal ions of MnII , CoII , NiII , CuII , ZnII , CdII and PdII with schiff base [(E)-1-((2-amino-5-(3, 4, 5-trimethoxybenzyl) pyrimidin-4-ylimino) methyl) naphthalen-2-ol [HL)]. The prepared [HL] was characterized by FT-IR, UV-Vis spectroscopy, 1H13CNMR spectra Mass spectra and melting point. The compounds were characterized by techniques UV-Vis and FT-IR spectral studies, micro analysis (C.H.N), determination of atomic absorption, chloride content, molar conductivity measurements, magnetic susceptibility and melting point. The ligand acts as a monobasic tridentate, coordinating through deprotonated phenolic O and azomethine N atoms. The compounds are neutral electrolytic in dimeth

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Publication Date
Sun Sep 01 2019
Journal Name
Baghdad Science Journal
A New Method for the Isolation and Purification of Trigonelline as Hydrochloride from Trigonella foenum-graecum L.
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Separation of Trigonelline, the major alkaloid in fenugreek seeds, is difficult because the extract of these seeds usually contains Trigonelline, choline, mucilage, and steroidal saponins, in addition to some other substances. This study amis to isolate the quaternary ammonium alkaloid (Trigonelline) and choline from fenugreek seeds (Trigonella-foenum graecum L.) which have similar physiochemical properties by modifying of the classical method. Seeds were defatted and then extracted with methanol. The presence of alkaloids was detected by using Mayer's and Dragendorff's reagents. In this work, trigonilline was isolated with traces of choline by subsequent processes of purification using analytical and preparative TLC techniques.

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Publication Date
Sun Dec 25 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Molecular Docking Study and Cytotoxicity Evaluation of some Quinazolinone Derivatives as Nonclassical Antifolates and Potential Cytotoxic Agents
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A series of new 4(3H)-quinazolinone derivatives (S1-S4) were synthesized and characterized   by FTIR,1HNMR and 13CNMR .Their cytotoxic activity against a set of human cancer cell lines MCF-7 (breast) and A549 (lung) was evaluated using MTT assay. To detect their selectivity toward cancer cells, the compounds were also tested against epithelial cells derived from normal human fibroblast (NHF). Methotrexate (MTX) was used as a reference for comparison . All the tested compounds exhibited toxicity against the normal cells lower than cancer cells. All the tested compounds displayed higher cytotoxicity against lung cancer cell line (A549) than MTX with the most

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Publication Date
Wed Oct 01 2025
Journal Name
Chinese Journal Of Analytical Chemistry
Synthesis, characterization, antioxidant and bioactivity assessment, and thermodynamic analysis of metal ion complexes using a novel azo dye
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Publication Date
Mon Dec 30 2013
Journal Name
Journal Of The College Of Basic Education
Synthesis and Antimicrobial Activities of (Mn, Co, Ni, Cu, Hg and Ag) Complexes with Poly (Vinyl-4-Aminobenzoate)
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The aim of this work is synthesis of _Eoly (Vinyl-4-AminoBenzoate) (PVAB) from reaction of _Eoly Vinyl Alkohol PVA with 4-aminobenzoyl chloride in alkaline media. We also prepare the metal complexes of poly (vinyl- 4-aminobenzoate) and antimicrobial properties were evaluated by dilute method against five pathogenic bacteria (Escherichia coli, Shigella dysentery, Klebsiella pneumonae, Staphylococcus aureus, Staphylococcus Albus) and two fungal (Aspergillus Niger, Yeast). All polymer metal complexes showed different activities against the various microbial isolates. The polymer metal complexes showed higher activity than the free polymer.

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Publication Date
Wed Apr 20 2016
Journal Name
International Journal Of Chemical Engineering And Applications
Synthesis, Characterization, and Anti-microbial Study of Polycyclicacetal Metal Complexes Derived from PEG and (Erythro-Ascorbic Acid) Derivative
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Polymer metal complexes of poly ethylene glycol acetal and Ag (I), Cu (II), Ni (II), Mn (II), Co (III) and Hg (II) were prepared from the reaction of PEG with aldehyde derived fromErythro-ascorbic acid (pentulosono-ɣ-lactone-2, 3- enedianisoate). All these compounds were characterized by Thin Layer Chromatography (TLC) and FTIR spectra and aldehyde was also characterized by (U.V-Vis), 1HNMR,13CNMR, and mass spectra. It has been established that, the polymer and its metal complexes showedgood activities against four pathogenic bacteria (Escherichia coli , Klebsiellapneumonae,Staphylococcusaureus, Staphylococcus Albus) and two fungal (Aspergillus Niger,Yeast). The polymer metal complexes showed higher activity than the free polymer.Theorder

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Publication Date
Fri Nov 03 2023
Journal Name
Karbala International Journal Of Modern Science
Synthesis and characterization of zirconium oxide nanoparticles using Z. officinale and S. aromaticum plant extracts for antibacterial application
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Publication Date
Fri Apr 01 2016
Journal Name
International Journal Of Chemical Engineering And Applications
Synthesis, Characterization, and Anti-microbial Study of Polycyclicacetal Metal Complexes Derived from PEG and (Erythro-Ascorbic Acid) Derivative
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Polymer metal complexes of poly ethylene glycol acetal and Ag (I), Cu (II), Ni (II), Mn (II), Co (III) and Hg (II) were prepared from the reaction of PEG with aldehyde derived from Erythro-ascorbic acid (pentulosono-ɣ-lactone-2, 3- enedianisoate). All these compounds were characterized by Thin Layer Chromatography (TLC) and FTIR spectra and aldehyde was also characterized by (U.V-Vis), 1HNMR,13CNMR, and mass spectra. It has been established that, the polymer and its metal complexes showed good activities against four pathogenic bacteria (Escherichia coli ,Klebsiellapneumonae, Staphylococcusaureus, Staphylococcus Albus) and two fungal (Aspergillus Niger,Yeast). The polymer metal complexes showed higher activity than the free polymer. The

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