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bijps-1233
Development, Characterization and Pharmacological Investigation of Umbelliferone Conjugates of NSAIDs
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The present investigation developed the ester prodrugs of Non-steroidal anti inflammatory drugs (NSAIDs), Mefenamic acid and Flurbiprofen by conjugating with the natural antioxidant, 4-methyl umbelliferone that resulted the formation of Mefenamic acid-umbelliferone ester prodrug and Flurbiprofen-umbelliferone ester prodrug .The principal objective this study is the synthesis of the ester prodrugs of NSAIDs with the enhanced therapeutic activity and minimized side effects. Prodrugs were synthesized by coupling method using N,N- dicyclohexylcarbodiimide/4-dimethylaminopyrimidine, subjected to  physical, chemical characterization, spectral characterization (IR, 1H NMR, 13C NMR and Mass spectra),hydrolysis-kinetic study and pharmacological evaluation such as anti-inflammatory, ulcerogenecity as well as the effect of the NSAIDs in the central nervous system against degenerative mechanisms. The current study revealed that the umbelliferone conjugates of NSAIDs which upon administration would release the parent drug as a result of enzymatic or non-enzymatic hydrolysis in the desired site with enhanced anti inflammatory activity and reduction in the gastro intestinal toxicity. Also the synthesized pordrugs showed enhanced brain targeting efficiency with protective action against the degenerative processes.

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Publication Date
Wed Nov 07 2018
Journal Name
Asian Journal Of Pharmaceutical And Clinical Research
INVESTIGATING THE EFFECT OF DIFFERENT GRADES AND CONCENTRATIONS OF PH‑SENSITIVE POLYMER ON PREPARATION AND CHARACTERIZATION OF LIDOCAINE HYDROCHLORIDE AS IN SITU GEL BUCCAL SPRAY
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Objective: The present study was aimed to develop a pH-triggered in situ gel for local release of lidocaine hydrochloride (lidocaine HCL) in the buccal cavity to improve the anesthetic effect of this amino amide drug which has very high water solubility. The formulations were introduced to the oral cavity as a spray to improve compliance and for easier administration.Methods: In this work, two grades of carbopol (934 and 940)-based in situ gel spray were designed. The formulations containing lidocaine HCl 5% were prepared by mixing different concentrations of carbopol with xanthan gum. Eight formulations were investigated and evaluated for gelation capacity, spray angle, volume of solution delivered per each actuation, rheological p

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Publication Date
Wed Nov 15 2023
Journal Name
Oncology And Radiotherapy
Synthesis, spectroscopic characterization, molecular docking, antioxidant and anticancer studies of some metal complexes from tetraazamacrocyclic Schiff base ligand
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Five novel nickel, iron, cobalt, copper, and mercury complexes were synthesized from tetraazamacrocyclic Schiff base ligand (L), which were derived from 3-(4-(dimethyl amino) benzylidene) pentane-2,4-dione and 1,2- diaminocyclohexane in a 2:2 molar ratio. Many physico-chemical and spectroscopic techniques, including melting point, 1HNMR, 13CNMR, elemental analysis, molar conductance, magnetic susceptibility, UV-Vis, FT-IR, and thermogravimetric analysis (TGA), were used to characterize the Schiff base ligand and all metal complexes. The octahedral geometry of all the complexes [MLCl2] is confirmed by spectroscopic analyses. All substances' biological properties, such as their in vitro antioxidant activity or level of free radical scavenging

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Publication Date
Thu Aug 28 2014
Journal Name
Iraqi National Journal Of Chemistry The Editorial Board
The New C-2,C-3 Substituted Heterocyclic Derivatives of L-Ascorbic acid: Synthesis, Characterization, and Bacterial Activity
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New Schiff bases derivatives [IV]a-e is prepared via condensation of Derythroascorbic acid with p-substituted aldehydes in dry benzene. To obtain these derivatives, the 5,6-O-isopropylidene-L-ascorbic acid[I] was chosen as starting material, compound prepared from the reaction of L-ascorbic acid as starting material. Compound[I] was prepared from the reaction of L-ascorbic acid with dry acetone in the presence of hydrogen chloride. The esterification of hydroxyl groups at C-2 and C-3 positions with excess ofethyl α –chloroacetate in the presence of sodium acetate produce acorresebonding ester [II] , which was condensed with hydrazine hydrate to give new hydrazide [III] . The new Schiff bases [IV]a-e were synthesized by reaction of acid h

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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
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Preparation, Characterization and Biological Evaluation of some Lanthanide (ΙΙΙ) ions Complexes with 3-(1-methyl-2-benzimidazolylazo)-Tyrosine
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A series of lanthanide metal (???) complexes have been prepared from the new azo ligand, 3-(1-methyl-2-benzimidazolylazo)-Tyrosine (MBT). The structural feature were confirmed on the basis of their elemental analysis, metal content, molar conductance, magnetic measurement, FTIR, 1 HNMR and UV-Vis spectra studies. The isolated complexes were found to have a mole ratio (1:2) (metal:ligand) stoichiometry with the general formula [Ln(MBT)2]Cl (Ln(???) = La, Ce, Pr, Nd, Sm, Eu and Gd). The chelates were found to have octahedral structures. The FTIR spectra shows that the ligand (MBT) is coordinated to lanthanide ions as a N, N, O-tridentate anion via benzimidazole nitrogen, azo nitrogen and oxygen of hydroxyl after deprotonation. Com

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Publication Date
Tue Sep 01 2020
Journal Name
Baghdad Science Journal
In Silico Characterization of a Cyclin Dependent Kinase -A (CDKA) and its Coding Gene in some Oryza Species
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Rice (Oryza sativa) is a fundamental food for the majority of world population. Cyclin Dependent Kinase -A (CDKA) accelerates transition through different stages of cell cycle and contributes in gametes formation. In the present investigation, a CDKA encoding gene along with the corresponding protein were characterized in O. sativa Indica Group, O. glaberrimaO. barthii, O. brachyantha, O. glumipatula, O. longistaminata, O. meridionalis, O. nivara, O. punctata and O. rufipogon using in silico analyses. The results reflected little variation in most species except O. longistaminata and O. brachyantha. Compared with the remaining species, O. longistaminata

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Publication Date
Wed Jun 03 2015
Journal Name
Baghdad
Synthesis, characterization and Antibacterial of 2, 3 Dihydrobenzo Thiazole -2- Carboxylic acid complexes with some selected Metal ions.
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Publication Date
Fri Sep 01 2023
Journal Name
International Journal Of Biological Macromolecules
Optimization and characterization of carrageenan/gelatin-based nanogel containing ginger essential oil enriched electrospun ethyl cellulose/casein nanofibers
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Publication Date
Mon Apr 01 2024
Journal Name
Iraqi Journal Of Applied Physics
Structural and Electrochemical Characterization of ITO Electrode Modified by f- MWCNT/graphene/polypyrrole Nanocomposite Decorated by Gold Nanoparticles
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There is currently a pressing need to create an electro-analytical approach capable of detecting and monitoring genosensors in a highly sensitive, specific, and selective way. In this work, Functionalized Multiwall Carbon Nanotubes, Graphene, Polypyrrole, and gold nanoparticles nanocomposite (f-MWCNTs-GR-PPy-AuNP) were effectively deposited on the surface of the ITO electrode using a drop-casting process to modify it. The structural, morphological, and optical analysis of the modified ITO electrodes was carried out at room temperature using X-ray diffraction (XRD), field emission scanning electron microscopy (FE-SEM) images, atomic force microscopy (AFM) and Fourier transform infrared (FTIR) spectra. Cyclic voltammetry (CV) and electrochemi

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Publication Date
Fri Sep 29 2017
Journal Name
Asian Journal Of Chemistry
Synthesis, Characterization of p-Nitrophenyl azo-β-Naphthyl- (4-Azobenzoic acid)-4-benzoate and its PVA-Grafting Polymer
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An aromatic ester containing two azo groups namely p-nitro phenyl azo-β-naphthyl-(4'-azobenzoic acid)-4-benzoate was synthesized by esterfiaction of 4,4'-azo dibenzoic acid with p-nitro phenyl azo-β-naphthol. Synthesized ester was characterized by CHN-Elemental analysis, FTIR, 1H NMR and 13C NMR. A modified PVA polymer was obtained by grafting 10 g of PVA-polymer via partial esterification with (2, 3, 4 g) p-nitro phenyl azo-1-naphthyl-4-azobenzoic acid)-4-azo benzoate. Grafting PVA-polymer behaviours was studied, by physical measurements (solubility, swelling), thermal properties (DSC) and tensile.