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.
Nimodipine (NMD) is a dihydropyridine calcium channel blocker useful for the prevention and treatment of delayed ischemic effects. It belongs to class ? drugs, which is characterized by low solubility and high permeability. This research aimed to prepare Nimodipine nanoparticles (NMD NPs) for the enhancement of solubility and dissolution rate. The formulation of nanoparticles was done by the solvent anti-solvent technique using either magnetic stirrer or bath sonicator for maintaining the motion of the antisolvent phase. Five different stabilizers were used to prepare NMD NPs( TPGS, Soluplus®, HPMC E5, PVP K90, and poloxamer 407). The selected formula F2, in which Soluplus
has been utilized as a stabilizer, has a par
... Show MoreNew Fourteen compounds were synthesized in four steps. The first step included synthesis of 2-biphenyl fused ring of imidazo(1,2- a)pyrimidine from the reaction of 2-aminopyrimidine and biphenyl phenacyl bromide . The second step was introduced aldehyde group from the reaction of 2-biphenyl fused rings of imidazo(1,2-a)pyrimidine with POCl3 in presence of DMF and CHCl3. 3-Carbaladehyde derivatives of fused imidazo/pyrimidine was reacted with different aromatic amines to afford new Schiff bases. These new 3- imines derivatives was reduced by using sodiumborohydride to yield another new 3-aminomethyl-2-biphenyl imidazo (1,2-a)pyrimidine derivatives in moderate yield .Some new prepared compounds were identified by melting point, FT- IR , 13C-
... Show MoreSome metal ions (Mn+2, Co+2, Ni+2, Cu+2, Zn+2, Cd+2 and Hg+2) complexes of quinaldic acid (QuinH) and α-picoline (α-Pic) have been synthesized and characterized on the basis of their , FTIR, (U.V-Vis) spectroscopy, conductivity measurements, magnetic susceptibility and atomic absorption. From the results obtained the following general formula has suggested for the prepared complexes [M(Quin)2( α-Pic)2].XH2O where M+2 = (Mn, Co, Ni, Cu, Zn, Cd and Hg), X = 2, X = zero for (Co+2 and Hg+2) complexes, (Quin-) = quinaldate ion, (α-Pic) = α-picoline. The results showed that the deprotonated ligand (QuinH) by using (KOH) coordinated to metal ions as bidentate ligand through the oxygen atom of the carboxylate group (-COO-) and the nitrogen ato
... Show MoreThis study including synthesis of some new Schiff bases compounds [1‐6] from the reaction of Sulfamethoxazole drug with some aromatic aldehydes in classical Schiff base method then treatment Schiff bases with succinic anhydride to get oxazepines rings [7-11]These derivatives were characterized by melting point, FT‐IR, 1H NMR and mass spectra. Some of synthesized compounds were evaluated in vitro for their antibacterial activities against three kinds of pathogenic strains Staphylococcus aureus, Escherichia coli
Incorporating waste byproducts into concrete is an innovative and promising way to minimize the environmental impact of waste material while maintaining and/or improving concrete’s mechanical characteristics and strength. The proper application of sawdust as a pozzolan in the building industry remains a significant challenge. Consequently, this study conducted an experimental evaluation of sawdust as a fill material. In particular, sawdust as a fine aggregate in concrete offers a realistic structural and economical possibility for the construction of lightweight structural systems. Failure under four-point loads was investigated for six concrete-filled steel tube (CFST) specimens. The results indicated that recycled lightweight co
... Show MoreTo move forward on the path of goodness and peace, we must realize that, in the midst of the great diversity of cultures and forms of human life in the world, that we form one human nation, which God Almighty created to worship Him on His earth and under His heavens and to enjoy His bounties and natural resources that God Almighty has bestowed upon that nation. On one land, and it is governed by one common destiny. Every country has been endowed with a natural resource by God Almighty that distinguishes it from the other country to live in prosperity if these wealth are distributed equally among the members of the same society and societal justice is achieved. We must join together to work for the establishment of a sustainable global commu
... Show MoreUrbanization can not be seen as a modern phenomenon. It has led people to live and live in cities for thousands of years. It should be noted here that the oldest villages and large cities have emerged after the crystallization of civilization, that the emergence of cities was one of the phenomena of civilization. There is no doubt that the cities after the emergence has contributed to the development of civilization effective contribution. There has been a civilizational progress when the man practiced agriculture and used metal tools and invented the wheels and went to write in the New Stone Age. In this period, many changes in the field have taken place in economic, cultural and social life. In the economic and cultural aspect, this tr
... Show MoreThe research is a vision of the future of industry in Iraq, so it is may be outside the ceiling of the capabilities of the Iraqi economy, and therefore it is exaggerated. Therefore, future plans must be applicable through the availability of capabilities. Everyone knows that the financial and administrative corruption and mismanagement of resources are the main cause of the inefficiency of the industrial sector, and the failure to exercise its real role in achieving economic development.; as well as the political situation and the dominance of parties and their insistence on addressing positions that have a strong relationship in managing the economic sector that has a significant impact on drawing the economic map in its current
... Show MorePlay constitutes a significant means for children to figure out the world around. Play helps children to have a healthy brain that increase their creativity via developing emotional, cognitive, physical strength. Thus, the current research aims to identify the role of play in psychological development of children. The findings of study revealed that play develops children’s cognitive, emotional abilities and enhances their self-confidence. Play forms a major approach for learning that promotes children to get rid of stress. Additionally, it supports language development of children
the regional and spatial dimension of development planning must be taken as a point of departure to the mutual of the spatial structure of the economy , development strategy and policies applied 'therein such as the location principles and regional development coordination of the territorial problems with the national development planning and timing of regional vis-a-vis national development plan_. Certain balance and integration is of sound necessity' between national _regional and local development objectives through which the national development strategy should have to represent the guidelines of the local development aspirations and goals. The economic development exerts an impact on the spatial evolution, being itself subje
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