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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 Aug 24 2023
Journal Name
Migration Letters
Imaginative Interconnection and its Relationship to Spatial Thinking Among Preparatory School Students in Mathematics
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Publication Date
Tue Jul 05 2022
Journal Name
Journal Of Pharmaceutical Care
Epidemiological and Clinical Factors Affecting the Response to Etanercept Among Patients with Rheumatoid Arthritis
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Publication Date
Thu Jun 01 2017
Journal Name
Journal Of Economics And Administrative Sciences
Proposed Entropy Loss function and application to find Bayesian estimator for Exponential distribution parameter
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The aim of this paper to find Bayes estimator under new loss function assemble between symmetric and asymmetric loss functions, namely, proposed entropy loss function, where this function that merge between entropy loss function and the squared Log error Loss function, which is quite asymmetric in nature. then comparison a the Bayes estimators of exponential distribution under the proposed function, whoever, loss functions ingredient for the proposed function the using a standard mean square error (MSE) and Bias quantity (Mbias), where the generation of the random data using the simulation for estimate exponential distribution parameters different sample sizes (n=10,50,100) and (N=1000), taking initial

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Publication Date
Wed Jan 01 2014
Journal Name
Al-adab Journal
Glottal Stop in R.P English and Standard Arabic with Reference to Some Other Varieties
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Publication Date
Sat Aug 21 2021
Journal Name
Engineering, Technology & Applied Science Research
A Comparison between Static and Repeated Load Test to Predict Asphalt Concrete Rut Depth
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Rutting has a significant impact on the pavements' performance. Rutting depth is often used as a parameter to assess the quality of pavements. The Asphalt Institute (AI) design method prescribes a maximum allowable rutting depth of 13mm, whereas the AASHTO design method stipulates a critical serviceability index of 2.5 which is equivalent to an average rutting depth of 15mm. In this research, static and repeated compression tests were performed to evaluate the permanent strain based on (1) the relationship between mix properties (asphalt content and type), and (2) testing temperature. The results indicated that the accumulated plastic strain was higher during the repeated load test than that during the static load tests. Notably, temperatur

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Publication Date
Fri Aug 01 2014
Journal Name
Journal Of Economics And Administrative Sciences
Comparison between the Local Polynomial Kernel and Penalized Spline to Estimating Varying Coefficient Model
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Analysis the economic and financial phenomena and other requires to build the appropriate model, which represents the causal relations between factors. The operation building of the model depends on Imaging conditions and factors surrounding an in mathematical formula and the Researchers target to build that formula appropriately. Classical linear regression models are an important statistical tool, but used in a limited way, where is assumed that the relationship between the variables illustrations and response variables identifiable. To expand the representation of relationships between variables that represent the phenomenon under discussion we used Varying Coefficient Models

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Publication Date
Fri Oct 01 2021
Journal Name
Theory And Practice In Language Studies
Critical Discourse Analysis and Rhetorical Tropes in Donald Trump’s First Speech to the UN
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Language and politics go hand in hand and learning and comprehending political genre is to learn a language created for codifying, extending and transmitting political discourse in any text/talk. Drawing upon the theoretical framework of Fairclough’s CDA and Rhetoric, the current study aims at investigating Donald Trump’s First Speech, from the point of frequency and functions of some rhetorical strategies (Parallelism, Anaphora and the Power of Three, Antithesis and Expletive, etc.), Nominalization, Passivization, We-groups and Modality as well as Lexical and Textual Analysis, presented to the UN delivered on Sep. 19, 2017. Specifically, the study seeks to determine: (1) how President Trump succeeded in conveying his notions an

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Publication Date
Sun Oct 01 2023
Journal Name
Minerva Dental And Oral Science
Salivary interleukin-1β as a biomarker to differentiate between periodontal health, gingivitis, and periodontitis
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Publication Date
Sat Jul 01 2023
Journal Name
Journal Of Engineering
Silica Fume Modified Cement-Based Mortar Exposed to High Temperatures: Residual Strengths and Microstructure
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Several previous investigations and studies utilized silica fume (SF) or (micro silica) particles as supplementary cementitious material added as a substitute to cement-based mortars and their effect on the overall properties, especially on physical properties, strength properties, and mechanical properties. This study investigated the impact of the inclusion of silica fume (SF) particles on the residual compressive strengths and microstructure properties of cement-based mortars exposed to severe conditions of elevated temperatures. The prepared specimens were tested and subjected to 25, 250, 450, 600, and 900 °C. Their residual compressive strengths and microstructure were evaluated and compared with control samples (C

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Publication Date
Tue Aug 04 2020
Journal Name
Indonesian Journal Of Pharmacy
Design and Synthesis of Novel Derivatives of 4-(6-(4-Substituted Phenyl)-7H-[1,2,4] Triazolo[3,4-b][1,3,4]Thiadiazin-3- yl) Phenol as a Potent Inhibitor of Tubulin with Antitumor Activity
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