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.
Coumarin derivatives have shown different biological activities, such as antifungal, antibacterial antiinflammatory, and antioxidant activities, besides antibiotic resistance modulating effects, and anti-HIV, hepatoprotective, and antitumor effect. So, new coumarin derivatives (hydrazones and an amide) were synthesized through multisteps reactions. All the synthesized target compounds were characterized by FT-IR spectroscopy, 1HNMR analysis. The compounds then evaluated for their anti-bacterial activity by means of well-diffusion method against two gram-positive bacteria (Staphylococcus aureus, Streptococcus pneumoniae) and two gram-negative bacteria (E.coli and Pseudomonas aeruginosa). The highest activity was demonstr
... Show MoreGold nanoparticles AuNPs have proven to be powerful tools in various nanomedicine applications, because of their photo-optical distinctiveness and biocompatibility. Noble metal gold nanoparticles was prepared by pulsed laser ablation method (1064-Nd: YAG with various Laser power from 200 to 800 mJ and 1 Hz frequency) in distil water. The process was characterized using UV-VIS absorption spectroscopy. Morphology and average size of nanoparticles were estimated using AFM and X-ray diffraction (XRD) analysis which show the nature of gold nanoparticles (AuNPs). Antibacterial activity of gold nanoparticles as a function of particles concentration against gram negative bacterium Escherichia coli and gram positive bacterial Staphylococcus aureu
... Show MoreTill now, isatin derivatives have received a lot of interest in organic and medicinal chemistry due to their significant biological and pharmacological activities. Schiff’s and Mannich bases of isatins are an effective group of heterocyclic derivatives that play a significant role in medicinal chemistry as antimicrobial agents. In light of these facts, new Schiff bases and Mannich bases of isatin were synthesized. The monomer Mannich bases; 3(a-e) have been synthesized by reacting isatin with different secondary amines, piperidine, morpholine, and pyrrolidine, dimethylamine, diphenylamine, separately, and formaldehyde, while the dimer (5) formed by using piperazine and formaldehyde which then react separately with Phenylhydrazine
... Show MoreThe issue of peace, renunciation of violence, and acceptance of the other is one of the vital issues that rose to the top of the list of priorities at the end of the last century and the beginning of the new millennium of the conscience of the Iraqi people by spreading the culture of peace. In this context, we seek during this research to identify the concept of the culture of peace and its impact on sustainable development, and to draw a set of results and suggestions to consolidate this culture in our Iraqi society as an obligation of sustainable development.
After the twenty – first century become necessary for us motorcade era in educational a chevements by searching for the best strategies and teaching methods and techniques artotalbagesh resorting to the strategy
Did not use in use in the teaching of the foreseeable material general by voice and teaching perspective for the student of the class fourth science
In particular ,so the researcher asking the question follows:
Can the peer education strategy to have an impact in perspective drawing skill development ?
From here it demonstrated the importance of current research know the impact of p
... Show MoreIn present work examined the oxidation desulfurization in batch system for model fuels with 2250 ppm sulfur content using air as the oxidant and ZnO/AC composite prepared by thermal co-precipitation method. Different factors were studied such as composite loading 1, 1.5 and 2.5 g, temperature 25 oC, 30 oC and 40 oC and reaction time 30, 45 and 60 minutes. The optimum condition is obtained by using Tauguchi experiential design for oxidation desulfurization of model fuel. the highest percent sulfur removal is about 33 at optimum conditions. The kinetic and effect of internal mass transfer were studied for oxidation desulfurization of model fuel, also an empirical kinetic model was calculated for model fuels
... Show MoreObjective: Schiff’s and Mannich bases of isatins are an important group of heterocyclic compounds which are of great importance in medicinal chemistry as antimicrobial agents. In the vision of these facts, new bis-Schiff bases and Mannich bases of isatins were synthesized. Methods: Three different bis-Schiff bases (3a-c) have been synthesized by reacting isatin, 5-fluoroisatin and 5-methoxy isatin with thiophene-2- carboxaldehyde using hydrazine hydrate to link between the carbonyl compounds, and then these bis- Schiff bases were condensed with two different secondary amines (piperidine and morpholine) separately, and formaldehyde to form the Mannich bases (4a-c and 5a-f), respectively. Results: The structures of the newly synthesized com
... Show MoreThis work introduces a new electrode geometry for making holes with high aspect ratios on AISI 304 using an electrical discharge drilling (EDD) process. In addition to commercially available cylindrical hollow electrodes, an elliptical electrode geometry has been designed, manufactured, and implemented. The principal aim was to improve the removal of debris formed during the erosion process that adversely affects the aspect ratio, dimensional accuracy, and surface integrity. The results were compared and discussed to evaluate the effectiveness of electrode geometry on the machining performance of EDD process with respect to the material removal rate (MRR,) the electrode wear rate (EWR), and the tool wear ratio (TWR). Dimensional features an
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