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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
Wed Jan 01 2020
Journal Name
Biochemical & Cellular Archives
ECO-FRIENDLY SYNTHESIS OF MAGNESIUM OXIDE NANOPARTICLES USING FICUS BENGHALENSIS LEAF EXTRACT AND ITS ANTI-LEISHMANIASIS ACTIVITY
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Scopus
Publication Date
Thu Aug 01 2024
Journal Name
Russian Journal Of Bioorganic Chemistry
Synthesis, Characterization of Different Five-Membered Heterocyclic Derivatives, Evaluated Their as Antioxidant, and In Vitro Antimicrobial Agents
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Objective:This study involved synthesis of a new series of different five-membered heterocyclic derivatives, testing their antioxidant activity, and examining their potential in vitro antimicrobial agents. Methods: The synthesis of the derivatives involved a three-step process. Initially, succinyl chloride was reacted with methanol, followed by a reaction with 80% hydrazine hydrate through a nucleophilic addition-elimination mechanism, resulting in the formation of succinohydrazide (I). This compound was then employed as a precursor for the synthesis of Schiff bases (II), and (III) by reacting it with m-nitro benzaldehyde and p-nitro benzaldehyde. Following this, a ring closure reaction was applied using thioglycolic acid, glycolic acid,

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Publication Date
Wed Nov 02 2016
Journal Name
Ibn Al-haitham Jour. For Pure & Appl. Sci.
Synthesis, Spectroscopic and Adsorption Studies of Cobalt (II) Complex for a ligand β-enaminone Derived from Sulfamethoxazole
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This paper concerns is the preparation and characterization of a bidentate ligand [4-(5,5- dimethyl-3-oxocyclohex-1-enylamino)-N-(5-methylisoxazol-3-yl) benzene sulfonamide]. The ligand was prepared from fusing of sulfamethoxazole and dimedone at (140) ºC for half hour. The complex was prepared by refluxing the ligand with a bivalent cobalt ion using ethanol as a solvent. The prepared ligand and complex were identified using Spectroscopic methods. The proposed tetrahedral geometry around the metal ions studied were concluded from these measurements. Both molar ratio and continuous variation method were studied to determine metal to ligand ratio (M:L). The M to L ratio was found to be (1:1). The adsorption of cobalt complex was carried out

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Publication Date
Sat Jul 20 2024
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis, Characterization of Nickel Cobaltite Nanoparticles and Its Use in Removal Methyl Green Dye from Aqueous Solution
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In this study, nickel cobaltite (NC) nanoparticles were created using the sol-gel process and used as an adsorbent to adsorb methyl green dye (MG) from aqueous solutions. The adequate preparation of nickel cobaltite nanoparticles was verified using FT-IR, SEM, and X-ray diffraction (XRD) studies. The crystalline particle size of NC nanoparticles was 10.53 nm. The effects of a number of experimental variables, such as temperature, adsorbent dosage, and contact time, were examined. The optimal contact time and adsorbent dosage were 120 minutes and 4.5 mg/L, respectively. Four kinetic models—an intraparticle diffusion, a pseudo-first-order equation, a pseudo-second-order equation, and the Boyd equation—were employed to monitor the adsorpti

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Publication Date
Fri Mar 01 2024
Journal Name
Baghdad Science Journal
First Transition Metal Complexes Salts of Diazonium Derived from Nitrogen Heterocyclic Compound, Synthesis, Characterization and Biological Activity
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Metal complexes chrome(III), manganese(II), iron(III), cobalt(II), nickel(II), cupper(II) and zinc(II) with diazonium of 3-amino-2-chloropyridine of general formula [2-Cl-C5H3N≡N]n[MXm], where n=2 or 3 for divalent and trivalent metal, m= 4 or 6  were synthesized. The complexes have been characterized by flame atomic absorption, (C.H.N), molar conductance, magnetic susceptibility UV-vis spectra, infrared spectra,1H-NMR spectroscopy and thermo gravimetric analysis (TGA and DTA). The measurements showed that the divalent metal ion complexes (M2+) have (1:2) M:L ratio with tetrahedral geometry around metal ions while the trivalent metal ions (M3+) formed (1:3) m

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of 5-Fluorouracil Derivatives as Possible Mutual Prodrugs with Meloxicam and Ibuprofen for Targeting Cancer Tissues
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In the present study, five derivatives have been designed to be synthesized as possible mutual prodrugs for 5-Fluorouracil (5-FU) and non steroidal anti-inflammatory drugs (NSAIDs) to selectively deliver the drugs into the cancer cells. The synthesis of the target compounds were accomplished following multistep reaction procedures, the chemical reaction followed up and the purity of the products were checked by TLC. The structure of the final compounds and their intermediates were confirmed by their melting points, infrared spectroscopy and elemental microanalysis, the hydrolysis of compound III was studied using HPLC technique. According to the results mentioned above, compounds (I−V) can be good candidates as possible mutual prod

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Publication Date
Fri May 01 2020
Journal Name
Journal Of Physics: Conference Series
Synthesis of Silver Nanoparticles by ecofriendly nvironmental method using Piper nigrum, Ziziphus spina-christi, and Eucalyptusglobulus extract
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Abstract<p>In the present study, silver nanoparticles (AgNPs) were prepared using an eco-friendly method synthesized in a single step biosynthetic using leaves aqueous extract of Piper nigrum, Ziziphus spina-christi, and Eucalyptus globulus act as a reducing and capping agents, as a function of volume ratio of aqueous extract(100ppm) to AgNO3 (0.001M), (1: 10, 2: 10, 3: 10). The nanoparticles were characterized using UV-Visible spectra, X-ray diffraction (XRD). The prepared AgNPs showed surface Plasmon resonance centered at 443, 440, and 441 nm for sample prepared using extract Piper nigrum, Ziziphus spina-christi, and Eucalyptus respectively. The XRD pattern showed that the strong intense peaks</p> ... Show More
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Publication Date
Sun Jun 01 2014
Journal Name
University Of Baghdad
New Analytical Methods for Drugs Analysis A Comparative Study
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Four different spectrophotometric methods are used in this study for the determination of Sulfamethoxazole and sulfanilamide drugs in pharmaceutical compounds, synthetic samples, and in their pure forms. The work comprises four chapters which are shown in the following: Chapter One: Includes a brief for Ultraviolet-Visible (UV-VIS) Absorption spectroscopy, antibacterial drugs and sulfonamides with some methods for their determination. The chapter lists two methods for optimization; univariate method and multivariate method. The later includes different types, two of these were mentioned; simplex method and design of experiment method. Chapter Two: Includes reaction of the two studied drugs with sodium nitrite and hydrochloric acid for diazo

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Publication Date
Sun Sep 01 2024
Journal Name
Baghdad Science Journal
Hetero-associative Memory Based New Iraqi License Plate Recognition
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نتيجة للتطورات الأخيرة في أبحاث الطرق السريعة بالإضافة إلى زيادة استخدام المركبات، كان هناك اهتمام كبير بنظام النقل الذكي الأكثر حداثة وفعالية ودقة (ITS) في مجال رؤية الكمبيوتر أو معالجة الصور الرقمية، يلعب تحديد كائنات معينة في صورة دورًا مهمًا في إنشاء صورة شاملة. هناك تحدٍ مرتبط بالتعرف على لوحة ترخيص السيارة (VLPR) بسبب الاختلاف في وجهة النظر، والتنسيقات المتعددة، وظروف الإضاءة غير الموحدة في وقت الحصول

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Publication Date
Fri Nov 01 2013
Journal Name
Journal Of Cosmetics, Dermatological Sciences And Applications
Podophyllin (10%) Ointment: A New Therapeutic Modality for Psoriasis
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KE Sharquie, AA Noaimi, WK Al-Janabi, Journal of Cosmetics, Dermatological Sciences and Applications, 2013

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