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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
Thu Mar 09 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Corrosion Inhibition of Aluminium in Acidic Medium using Amino Acid (Methionine)
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  Corrosion behavior of aluminium in 0.6 mol. dm-3 NaCl solution in acidic medium 0.7 was investigated in the absence and presence of different concentrations of amino acid, methionine, as environmentally – friendly corrosion inhibitor over temperature range (293-308)K. The investigation involved electrochemical polarization method using potentiostatic technique and optical microscopy, the inhibition efficiency increased with an increase in inhibitor concentration but decreased with increase in temperature. Results showed that the inhibition occurs through adsorption of the inhibitor molecules on the metal surface and it was found to obey Langmuir adsorption isotherm. Some thermodynamic parameters ∆. and activation ener

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Publication Date
Tue Jan 01 2013
Journal Name
Iraqi Journal Of Cancer And Medical Genetics
Apoptotic Activity of methionine γ- lyase on several cancer cell lines
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The apoptotic activity of methionine γ- lyase from Pseudomonas putida on cancer cell lines was indicated by measuring the concentration of cytochrome c in the supernatants of cell lines. The result revealed high concentration of cytochrome c in the supernatants of cancer cell lines (RD, AMGM and AMN3) respectively while the concentration of anti-apoptotic protein (Bcl-2) was very low.

Publication Date
Mon Jun 03 2019
Journal Name
Journal Of Global Pharma Technology
New Diquinazoline Derivatives: Synthesis and Evaluation of AntiBacterial Activi
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Oxazine and quinazoline has a very important in organic chemistry especially in hetero cyclic fields. this research consist the preparation of 4H,4'H-2,2'-bibenzo[d][1,3]oxazine-4,4'-dione compound (1) from di acid chloride with 2-aminobenzoic acid in pyridine as solvent to give compound (2) 3,3'-diamino-2,2'- biquinazoline-4,4'(3H,3'H)-dione .compound 2 include free amino group .this compound was reacted with maleic and phthalic anhydride for synthesized of cyclic imide compounds (3,4).another reaction for compound 2 with some substituted aromatic aldehyde for prepared of some novel Schiff bases (5-9) contains quinazoline ring. compound 1 was treated with sulfathiazole and sulfadiazine for synthesized of sulfa compounds contains sulf

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Publication Date
Sun Apr 23 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and antimicrobial evaluation of new 1,3,4 – Thiadiazole Derivatives
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The amino thiadiazole [I] on treatment with aromatic aldehydes yielded Schiff bases [IIa-c] , which cyclized to thiazolidinone [IIIa-c] derivatives by reaction with thioglycolic acid .Reaction of carbon disulfide and methyl iodide with [I] gavedithiomethyl[IV] which on treatment with o-phenylenediamine gave the condensed N-Imidazolythiadiazolylamine [V] , However , reaction of [I] with phenylisocyanate and phenylisothiocyanate afforded the carbamideand carbothiamide derivatives[VI.VII]a-c. The structure of these compounds was characterized from their  melting point , FTIR spectroscopy and elementalanalysis

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Publication Date
Sat Jun 03 2023
Journal Name
Iraqi Journal Of Science
Synthesis and Characterization of Some New Derivatives From 2-Mercaptobenzoxazole
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In this work 2-mercaptobenzoxazole (2-MBO) (1), was prepared by using homemade Auto clave .The synthesis involve treatment of 2-MBO with 2-chloro acetyl chloride to give 2-chloroacetyl thio benzoxazole (2), the product was treated with phenyl hydrazine to give 2-phenyl hydrazide acetyl thio benzoxazole (3). The new derivatives (4-13) were synthesized by reaction of 2-phenyl hydrazide acetyl thio benzoxazole (3) with different aromatic aldehydes in the presence of acetic acid. The compound (2) was treated with hydrazine hydrate to give product (14) then treated with different aromatic aldehydes in the presence of glacial acetic acid to give Schiff bases derivatives (15-24). Structure of all the prepared compounds confirmation were proved

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Publication Date
Fri Jun 24 2022
Journal Name
Iraqi Journal Of Science
Synthesis and Curing of New Phenolic Resins Containing Pendant TetrachloroPhthalimides
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Four new phenol-formaldehyde resins containing tetrachlorophthalimides in their repeating units were synthesized via condensation of formaldehyde with N-(hydroxy phenyl)tetrachlorophthalimides under conditions similar to those used in novolac preparation. In this work structural modifications were performed first via design and synthesis of new phenolic component represented by phenolic ring linked to thermally stable tetrachlorophthalimide moiety which condense with formaldehyde and second via introducing of phenolic hydroxyl groups present in the new synthesized resins by esterification reaction with acetyl chloride producing the corresponding acetoxy substituted resins. Both the prepared and the cured resins have new properties which

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Publication Date
Mon Apr 24 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of New Heterocyclic Derived from Pyromellitic Dianhydride
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  In this work two moles of 2-amino benzothiazole were allowed to react with one mole of pyromellitic dianhydride to produce N,N‾-Bis-(benzathiazol-2-yl) pyromellitamic diacid [I] which was submitted to esterification via the reaction with dimethyl sulphate in sodium carbonate in acetone as a solvent to synthesize N,N‾-bis-(benzothiazol-2-yl) pyromellitam diacetate [II] .This ester  was used to produce  novel  compounds through  two paths :- Path one:- Reaction of ester [II] with hydrazine in ethanol as a solvent to form the corresebonding  N,N‾-bis (benzothiazole-2-yl) –pyromellitamic acid hydrazide [III] which react with acetyl acetone in ethanol or with phthalic anhydride in dioxa

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Publication Date
Fri Nov 24 2023
Journal Name
Iraqi Journal Of Science
Synthesis and characterization of some New Derivatives from 2- Mercaptobenzothiazole
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In this work 2- mercaptobenzothiazole ( 2-MBT ) and some of its derivatives(1, 14 ,27) were prepared by using home made Auto clave .The synthesis involve treatment of 2- MBT or some of its derivatives with chloro acetyl chloride to give 1- chloro acetyl -2- MBT or the corresponding derivatives (2,15,28) . the product was treated with phenyl hydrazine to give the phenyl hydrazide derivatives (3,16,29) . The new derivatives(4-13, 17-26,30-39) were synthesized by reaction of the phenyl hydrazide derivatives with different aromatic aldehydes in the presence of Acetic Acid . Structure of all the prepared compounds confirmation were proved using FTIR , elemental analysis (C .H .N .S ) in addition to melting points.

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Publication Date
Mon Aug 07 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Preliminary Pharmacological Evaluation of Some New Triazole Derivatives
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  On the basis of the results which was previously obtained from the structural and the theoretical studies on ~-adrenergic drugs, a series of 2-propanolamine derivatives containing triazole moiety have been prepared and evaluated for their cardiovascular activity . These derivatives were tested by using spontaneously-beating right atria of albino rats.

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Publication Date
Fri Jun 24 2022
Journal Name
Iraqi Journal Of Science
Synthesis and Curing of New Phenolic Resins Containing Pendant TetrachloroPhthalimides
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Four new phenol-formaldehyde resins containing tetrachlorophthalimides in their repeating units were synthesized via condensation of formaldehyde with N-(hydroxy phenyl)tetrachlorophthalimides under conditions similar to those used in novolac preparation. In this work structural modifications were performed first via design and synthesis of new phenolic component represented by phenolic ring linked to thermally stable tetrachlorophthalimide moiety which condense with formaldehyde and second via introducing of phenolic hydroxyl groups present in the new synthesized resins by esterification reaction with acetyl chloride producing the corresponding acetoxy substituted resins. Both the prepared and the cured resins have new properties which

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