Preferred Language
Articles
/
bijps-577
Synthesis of New Opioid Analgesic Peptide Analogues to Enkephalin (Leucine- and Methionine-Enkephalin)
...Show More Authors

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

Crossref
View Publication Preview PDF
Quick Preview PDF
Publication Date
Sun Dec 25 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Atimicrobial Evaluation of Deuterated Analogues of Metronidazole
...Show More Authors

The discovery of novel therapeutic molecules is always difficult, and there are a variety of methodologies that use the most diverse and innovative medicinal chemistry approaches. One such approach is the deuteration technique: Deuteration is the process of substituting deuterium for hydrogen in a molecule. When compared to the drug molecule, its deuterated analogues may retain the features of the original molecule and, in some cases, improve its pharmacological activity, with fewer side effects and lower toxicity. Metronidazole is a commonly used antibiotic to treat anaerobic bacterial infections, protozoal and microaerophilic bacterial infections. Met

... Show More
View Publication Preview PDF
Scopus (2)
Crossref (2)
Scopus Crossref
Publication Date
Wed Feb 08 2023
Journal Name
Iraqi Journal Of Science
Synthesis of novel Nucleoside Analogues from Imidizoline and Evaluation their Anti microbial Activity
...Show More Authors

In this research some new nucleoside analogues were synthesized. Starting from α-D- glucose which was protected to glucose penta acetat α-D- glucose pyronside (1). Which was converted to active form 1-bromo protected sugar (2) as a sugar moiety. The base moiety 2-substituted imidazoline (3,4) was prepared from condensation of ethylene diamine with two kind of aromatic aldehydes, which were subjected to amino alkylation via Mannich reaction forming new nucleaobase derivatives (5-10). Condensation of nucleobase with bromo sugar through nucleophilic substitution of anomeric carbon with nitrogen forming new protected nucleoside analogues (11-16). De blocking of these nucleoside analogues with sodium methoxide in methanol afforded our targe

... Show More
View Publication Preview PDF
Publication Date
Wed Aug 02 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis of 3-C-Spiro Ring Nucleoside Analogues, of Possible Biological Activity
...Show More Authors

In this study, new derivatives of 3-C-spiro ring nucleoside analogues were synthesized. The structures of these derivatives were characterized by infrared spectroscopy,1HNMR (some of them) and elemental analysis. The nucleoside derivatives were tested for inhibition of E-coli and were all found to be active.

View Publication Preview PDF
Publication Date
Fri Jan 01 2021
Journal Name
Materials Today: Proceedings
Synthesis of gamma biguanides butyric acid analogues as HDAC inhibitors and studying their cytotoxic activity
...Show More Authors

View Publication
Scopus (5)
Crossref (4)
Scopus Clarivate Crossref
Publication Date
Sun Dec 30 2012
Journal Name
Al-kindy College Medical Journal
Analgesic Effect of Melatonin in Mice
...Show More Authors

Background: Melatonin is the main hormone secreted by the pineal gland. This indole compound (N-acetyl-5-methoxytryptamine) is derived from serotonin after two biochemical steps. Melatonin has been implicated in some pharmacological effects including sedative/hypnotic, anticonvulsant activity and others. The aim of this study was to investigate the antinociceptive effect of different doses of melatonin administered i.p. to mice, and then, to find the dose- response line of melatonin in mice as analgesic agent.
Methods: The dose response effect of melatonin (10, 50, and 100mg/kg) were assessed against control using tail flick test in mice as a model of nociceptive pain. In this model, all doses of melatonin were given intraperitoneally

... Show More
View Publication Preview PDF
Publication Date
Sun Nov 08 2015
Journal Name
مجلة كلية التربية الاساسية القاجسية
Synthesis, Characterization, and Antibacterial Properties of mixed ligand Complexes of (L-Leucine and 8-hydroxyquinoline) with some metals Ions
...Show More Authors

Publication Date
Fri Jun 30 2023
Journal Name
Iraqi Journal Of Science
Synthesis, Modification and Characterization of New Phenolic Resins linked to Tetrabromophthalimide
...Show More Authors

     The present work aimed to synthesize new phenol resins via incorporation of structural modification through introducing new phenolic compounds containing cyclic imide moiety in reaction with formaldehyde. The synthesis of these new resins involved three steps. First, one of the three N-(hydroxyphenyl)tetrabromophtalamic acids 1-3 were processed via a reaction between tetrabromophthalic anhydride and aminophenols. Amic acids 1-3 were dehydrated in the second step by smelting, producing the identical N-(hydroxyphenyl)tetrabromophthalimides 4-6. The new imides represent the new phenolic component

... Show More
View Publication Preview PDF
Scopus Crossref
Publication Date
Sat Apr 01 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of 3 - 3 - gem - di - C -Nitromethyl Nucleoside Analogues of Possible Biological Activity
...Show More Authors

Synthesis of new nucleoside analogues of the type : 3¢ , 3¢ - gem – di – C – nitromethly , expected to have useful application in the chemotherapeutic treatment of AIDS , cancer and microbial infections. The synthesis involved the condensation of the appropriate sugar derivative ( i.e . 3¢ , 3¢ –  gem – di – C – nitromethly – 1–  ribofuranose ) with nitrogen bases , such as , uracil and theophllin following a multi step scheme starting from diacetone golucose (1) (scheme 1) .The prepared compound were identified by spectroscopic methods ; ir , mass , 1H and 13C nmr.

View Publication Preview PDF
Crossref
Publication Date
Thu Aug 01 2013
Journal Name
Biochemistry
Mechanistic Insights from the Binding of Substrate and Carbocation Intermediate Analogues to Aristolochene Synthase
...Show More Authors

View Publication
Crossref (58)
Crossref
Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis and Evaluation of Antimicrobial activity of several new Maleimides to Benzothiazole moiety
...Show More Authors

In this work, a series of new maleimides linked to substituted benzothiazole moiety were synthesized. Synthesis of these new cyclic imides were performed via three steps, the first one involved preparation of a series of 2-aminobenzothiazole substituted with different substituents via reaction of different primary aromatic amines with ammonium thiocyanate and bromine in glacial acetic acid. The prepared 2- amino benzothiozoles were introduced in the second step in reaction with maleic anhydride producing a series of N-(substituted benzothiazole-2-yl) maleamic acids.The resulted maleamic acids were dehydrated in the third step via treatment with acetic anhydride and anhydrous sodium acetate to afford a series of the desirable N-(substitu

... Show More
View Publication Preview PDF
Crossref