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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
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis and Evaluation Antibacterial Activity of Some New Substituted 5-Bromoisatin Containing Five, Six Heterocyclic Ring
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This research includes the synthesis of some new different heterocyclic derivatives of 5-Bromoisatin. New sulfonylamide, diazine, oxazole, thiazole and 1,2,3-triazole derivatives of 5-Bromoisatin have been synthesized. The synthesis process started by the reaction of 5-Bromoisatin with different reagents to obtain schiff bases of 5-Bromoisatin intermediate compounds(1, 8, 19) by using glacial acetic acid as a catalyst in three routes. The first route, 5-Bromoisatin reacted with p-aminosulfonylchloride to product compound(1), then converted to sulfonyl amide derivatives(2-7) by the reaction of compound(1) with different substituted primary aromatic amine in absolute ethanol. The second route includes the reaction of 5-Bromoisatin rea

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Publication Date
Thu Feb 01 2018
Journal Name
Journal Of Pharmacy Research
Synthesis and antimicrobial evaluation of new-[2-amino-4- (4-chloro-/4-bromophenyl)-1,3-thiazole derivatives
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Publication Date
Wed Jun 26 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Acute Anti-inflammatory Evaluation of New Mefenamic Acid Derivatives Having 4-Thiazolidinone Nucleus
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Mefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug's potential side effects, new series of 4-t

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Publication Date
Fri May 01 2015
Journal Name
Ieee Transactions On Microwave Theory And Techniques
On the Design of Gyroelectric Resonators and Circulators Using a Magnetically Biased 2-D Electron Gas (2-DEG)
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Publication Date
Wed Nov 01 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation and characterization of Posaconazole as a Nano-micelles using d-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS)
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It is important to note that Posaconazole (POCZ) is a newly developed extended-spectrum triazole that belongs to BCS class II and has a solubility of less than 1µg/ml. In patients with a weakened immune system, POCZ has been shown to be effective as an antifungal treatment for invasive infections caused by candida and aspergillus species. The nano-micelles technique can be used to increase POCZ solubility. In order to increase their apparent solubility in water, nano-micelles are made by combining macromolecules that self-assemble into ordered structures capable of entrapping hydrophobic drug molecules in the interior domain. Dispersed colloidal systems, of which nano-micelles are a subset, are a large and diverse group. Composed of a p

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Publication Date
Fri Sep 15 2023
Journal Name
Sumer 2
Predictive value of C-reactive protein, D-dimer, Hemoglobin and Lactate dehydrogenase levels in diagnosing COVID-19 patients
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Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) has caused enormous issues worldwide and is the most infectious pandemic. This study included 50 subjects (evenly distributed between sexes) and their range of ages starting from 2 to 67 years. According to the study's result, the ages and genders of subjects include susceptibility to COVID-19. Males were found to be more infected than females, and the ages of 36 to 67 were more common than other age ranges. Also, BMI calculations revealed that male patients with COVID-19 have the highest percentage of obesity. The clinical parameter results have been found serum C‐reactive protein (CRP) as an essential indicator that changes significantly in infection with COVID‐19 an

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Publication Date
Wed Jan 01 2020
Journal Name
Systematic Reviews In Pharmacy
Synthesis of New Ibuprofen Derivatives Containing (Oxothiazolidin-3-yl) Amino Moiety with Expected Biological Activity
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Nonsteroidal anti-inflammatory drugs (NSAIDs) are drugs that help reduce inflammation, which often helps to relieve pain. In this research new ibuprofen oxothiazolidnone derivatives were synthesized from the reaction of Schiff base derivatives of Ibuprofen with mercapto acetic acid VI a-c, to improve the potency and to decrease the drug's potential side effects, a new series of 4-thiazolidinone derivatives of ibuprofen was synthesized VI a-c . The characterizations of the compounds were identified by using FTIR, 1HNMR technique and by measuring the physical properties.

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Publication Date
Thu Oct 01 2020
Journal Name
Biochem. Cell. Arch
NEW ORGANOTIN(IV) COMPLEXES DERIVED FROM 3,4-DIHYDROXYBENZALDEHYDEN(4)-ETHYL-3-SEMICARBAZONE LIGAND: SYNTHESIS, CHARACTERISATION AND BIOLOGICAL ACTIVITY
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Two new organotin(IV) complexes Me2Snesc (C1) and Bu2Snesc (C2) have been synthesised from the reaction of the corresponding organotin(IV) chloride with the Schiff base ligand 3,4-dihydroxybenzaldehyde-4-ethylsemicarbazone (H2esc). The ligand was prepared in two steps. The first step includes the formation of 4-ethylsemicarbazide, which then reacted with 3,4-dihydroxybenzaldehyde to give the title ligand. Complex formation between the organotin(IV) moiety and the anionic form of 3,4-dihydroxybenzaldehy-4-ethylsemicarbazone occurred through the o-dihydroxy positions. The ligand and its complexes were characterised by elemental analysis, FT-IR and NMR (1H, 13C and 119Sn) spectroscopy. Accordingly, the complexes were proposed to have tetrahedr

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Publication Date
Thu May 02 2013
Journal Name
Al-mustansiriyah
Synthesis, Spectroscopic and Biological Studies of a New some Complexes with N-Pyridine-2-Y1 methyl-benzene-1, 2-diamine.
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Publication Date
Sun Jul 09 2023
Journal Name
Journal Of Engineering
Effect of Allowable Vertical Load and Length/Diameter Ratio (L/D) on Behavior of Pile Group Subjected to Torsion
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Some structures such as tall buildings, offshore platforms, and bridge bents are subjected to lateral loads of considerable magnitude due to wind and wave actions, ship impacts, or high-speed vehicles. Significant torsional forces can be transferred to the foundation piles by virtue of eccentric lateral loading. The testing program of this study includes one group consists of 3 piles, four percentages of allowable vertical load were used (0%, 25%, 50%, and 100%) with two L/D ratios 20 and 30, vertical allowable load 110 N for L/D = 20 and 156 N for L/D = 30. The results obtained indicate that the torsional capacity for pile group increases with increasing the percentage of allowable vertical load, when the percentage of allowable vertica

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