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.
A series of 4-(methylsulfonyl)aniline derivatives were synthesized in order to obtain new compounds as a potential anti-inflammatory agents with expected selectivity against COX-2 enzyme. In vivo acute anti-inflammatory activity of the final compounds 11–14 was evaluated in rat using an egg-white induced edema model of inflammation in a dose equivalent to 3 mg/Kg of diclofenac sodium. All tested compounds produced significant reduction of paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the activity of compounds 11 and 14 was significantly higher than that of diclofenac sodium (at 3 mg/Kg) in the 120–300 minute time interval, while compound 12 expressed a comparable effect to that of di
... Show MoreMefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug's potential side effects, new series of 4-t
... Show MoreThe economy of a city has an important role not only in its establishment but also in its development. This is quite clear in the city of Baghdad throughout its history since its building in 762 A.D. In addition, most of its problems that the city is suffering from are basically related to not giving enough importance to the economic factors in the master planning of Baghdad since 1950’s. This may explain the failiars of master plans in dealing with the actual population growth and the city's inability to absorb such increases and interrelated and diverse activities which are negatively reflected on the economic variables particularly the effect on the land values, and the strong competitions amongst the land uses without previ
... Show MoreSickle cell disease (SCD) is a hereditary ailment that can cause severe pain and suffering to people who are affected. However, with continued investment in research and treatment options, we can make progress towards improving the lives of those with SCD. Over 40% of patients experience painful vaso-occlusive crises (VOCs), so we must work towards finding solutions and providing support for those living with this condition, These episodes, a hallmark of SCD, significantly contribute to morbidity, mortality, and a diminished quality of life, while also incurring substantial healthcare costs. Chronic pain particularly affects older adolescents and adults with SCD, with over half reporting daily discomfort. Opioid-based analgesics, though sti
... Show MoreMany pharmaceutical molecules have solubility problems that until yet consist a hurdle that restricts their use in the pharmaceutical preparations. Lacidipine (LCDP) is a calcium-channel blocker with low aqueous solubility and bioavailability.
Lipid dosage forms are attractive delivery systems for such hydrophobic drug molecules. Nanoemulsion (NE) is one of the popular methods that has been used to solve the solubility problems of many drugs. LCDP was formulated as a NE utilizing triacetin as an oil phase, tween 80 and tween 60 as a surfactant and ethanol as a co-surfactant. Nine formulas were prepared, and different tests performed to ensure the stability of the NEs, such as thermodyna
... Show MoreThe moisture sorption isotherms of Mefenamic acid tablets were investigated by measuring the experimental equilibrium moisture content (EMC) using the static method of saturated salt solutions at three temperatures (25, 35, and 45°C) and water activity range from 0.056 to 0.8434. The results showed that EMC increased when relative humidity increased and the sorption capacity decreased, the tablets became less hygroscopic and more stable when the temperature increased at constant water activity. The sorption curves had a sigmoid shape, type II according to Brunauer’s classification. The hysteresis effect was significant along with the whole sorption process. The results were fitted to three models: Oswin, Smith, and Guggen
... Show MorePrediction of daily rainfall is important for flood forecasting, reservoir operation, and many other hydrological applications. The artificial intelligence (AI) algorithm is generally used for stochastic forecasting rainfall which is not capable to simulate unseen extreme rainfall events which become common due to climate change. A new model is developed in this study for prediction of daily rainfall for different lead times based on sea level pressure (SLP) which is physically related to rainfall on land and thus able to predict unseen rainfall events. Daily rainfall of east coast of Peninsular Malaysia (PM) was predicted using SLP data over the climate domain. Five advanced AI algorithms such as extreme learning machine (ELM), Bay
... Show MoreTo synthesize new hydrazone derivatives of naproxen with enhanced anti-inflammatory activity and devoid the ulcerogenic side effects. Hydrazones were synthesized by conjugation of naproxen hydrazide with seven natural and synthetic aldehyde and ketone by using glacial acetic acid as catalyst. The synthesis has been carried out following simple methodology in excellent isolated yields.The structure of the synthesized derivatives has been characterized by elemental microanalysis (CHN), FTIR Spectroscopy, and other physicochemical properties.The anti- inflammatory activity of the synthesized compounds was evaluated in vivo using the egg-white induced edema model in rats, and the results of the biological assay was found to be comparable to Nap
... Show Morethe history of the Scouting movement reflects the global social cultural and technological change over more than a century. scouting aims to develop young people worldwide through educational programs based on specific principles and values. in arab countries, the scouting movement is considered one of the most important platforms contributing to developing young people and enhancing their rule. positive in society, began with the establishment of the first Scout camp in the region and witnessed great growth and prosperity over the decades the research reveals the historical roots and development of the scout movement in the leading arab countries and analyzes the positive impact of scout movement in the leading arab countries on the develo
... Show MoreThis research shows the problem of the economic development of underdeveloped countries in an unconventional way, as these papers explain the problems of the economic development. This research not only reviews the problems, but it illustrates them in a philosophical way, basis of the data of modernity, this mean it is a process of connecting between the absence of the modernity values and the failure of development in underdeveloped countries. The Search follows the descriptive approach to get to the goal of search by four main axes. The first axis includes clarifying modernity and its principles, the second axis includes clarifying the economic development , the third axis includes the features of the mod
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