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.
This paper addresses the nature of Spatial Data Infrastructure (SDI), considered as one of the most important concepts to ensure effective functioning in a modern society. It comprises a set of continually developing methods and procedures providing the geospatial base supporting a country’s governmental, environmental, economic, and social activities. In general, the SDI framework consists of the integration of various elements including standards, policies, networks, data, and end users and application areas. The transformation of previously paper-based map data into a digital format, the emergence of GIS, and the Internet and a host of online applications (e.g., environmental impact analysis, navigation, applications of VGI dat
... Show MoreTechnological development intersects with terrorism to a large extent, beyond the use of the Internet and social media, in order to spread ideas, obtain support and financing, and recruit new elements, to the area of tactics and techniques of terrorist attacks, and everything related to the arsenal of terrorist weapons in the present and future, while technology offers many benefits. In various fields, and contribute to achieving multiple gains for humanity, they provide extremist and terrorist organizations and elements with a set of weapons and means through which they attempt to bypass monitoring and control efforts and the restrictions imposed on the use of weapons. They also help in planning and implementing their terrorist operations,
... Show MoreEducational Planning, it's Importance in the Social, Economical and Educational Development
Financial crisis is one of the topics that have attracted the interest of researchers in recently. The research focused on the issue of the crisis of the Asian Tigers and the mortgage crisis and comparing them in terms of causes and repercussions. It may meet most of the financial crises in many of its causes, factors, roots and results in the advanced and the developing countries. This crisis has its own pattern and its causes and nature and it is characterized by a crisis of cash liquidity and the collapse of many banks and declare bankruptcy and a sharp decline in stock prices and indices of the stock market and so far the common denominators among the causes but does not mean this There are differences between the financial c
... Show MoreIn this study, new heterocyclic compounds were synthesized through the cyclization reactions of o-phenylenediamine (1) with various organic reagents. Benzodiazepine derivatives (2-4) were obtained by reaction of (1) with ethylacetoacetate, malonic acid and acetyl acetone.Treatment of compound (1) with chloroacetamide, chloroacetic acid, p-bromophenacyl bromide and oxalic acid dihydrate afforded quinoxaline derivatives (5-8), respectively. Reaction of compound (1) with benzoic acid, piperonal, cyclohexanone and carbon disulfide resulted in the formation of compounds (9-12), respectively. Finally, reaction of compound (12) with chloroacetic acid in the presence of potassium hydroxide produced compound (13).
Salicylaldehyde was react with 4-amino-2,3-dimethyl-1-phenyl-3-pyrazoline-5-on to produce the Schiff base ligand 2,3-dimethyl-1-phenyl-4-salicylidene-3-pyrazoline-5-on (L). The prepared ligand was identified by Microelemental Analysis, and FT.IR, UV-Vis spectroscopic techniques. A new complexes of Fe(III),Co(II),Ni(II),Cu(II),Ce(III) and Pb(II) with mixed ligands of dithizone (DTZ) and Schiff base were prepared in aqueous ethanol with a 2:2:1 M:L:DTZ. The prepared complexes were characterized using flame atomic absorption, (C.H.N) Analysis, FT.IR and UV-Vis spectroscopic methods as well as magnetic susceptibility and conductivity measurements. In addition biological activity of the ligands and complexes against two selected type of bacteria
... Show MoreSynthesis, Characterization And Biological Evaluation of Schiff Base And Ligand Metal Complexes of Some Drug Substances
Objective: This study involved the synthesis of new Schiff bases and 1,3-oxazepine derivatives from the baclofen drug and study the anticancer activities. Methods: Baclofen was initially reacted with aromatic aldehydes to create Schiff base derivatives (Ia–Ib), which were then closed in the next step using anhydrous acids to form oxazepine derivatives (IIa–IId). Results: The title compounds were synthesized successfully and identified using FT-IR, 1H NMR, and 13C NMR spectroscopy. Additionally, compound (IIc)’s (3-(4-chloro-phenyl)-4-[2-(4nitro-phenyl)-4,7-dioxo-4,7-dihydro-[1,3] oxazepin-3-yl]butyric acid) anticancer activity was assessed using MTT assay against FTC-133 (thyroid cancer) compared with WRL-68 (normal cell line). Discus
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