Non-steroidal anti-inflammatory drugs (NSAIDs) contain free –COOH which thought to be responsible for the GI irritation associated with all traditional NSAIDs. The esterification of this group is one of an approach to ultimate aim for reduce the gastric irritation; so in this study we synthesized and preliminarily evaluated new ester compounds as new analogues with expected selectivity toward COX-2 enzyme. Synthetic procedures have been successfully developed for the generation of the target compounds (III a and b). The synthetic approach involved multi-steps procedures which include: Synthesis of 4-hydroxy benzene sulphonamide ( I b ), synthesis of Naproxen and Ibuprofen acyl chloride and then reacting them with 4-hydroxy benzene sulphonamide to form final compounds ( III a-b) .The structures of these compounds were identified and characterized using (TLC), infrared spectroscopy (FT-IR), 1H NMR data and microanalysis (CHN).Pharmacological study as anti-inflammatory activities for the final compounds were studied in rats by induced edema type of inflammation. Moreover, the results of a docking study of compounds III a-b into the COX-2 binding site revealed that its mechanism was possibly similar to that of naproxen, a COX-2 inhibitor. The effect of them on COX-2 antibody was showed it could significantly inhibit COX-2 activity.
In The Name of Allah Most Gracious Most Merciful
This is a study dedicated to explaining the conditions of the end of heaven, stage by stage; And to draw the final picture of it, through the facts of the Qur’an, and to make the contextual integration of the verses of the end of heaven, and their arrangement in an intentional arrangement, a path that guides us to knowing the integrated picture of it on the Day of Resurrection, according to scientific interpretation.
The importance and usefulness of the research lies in:
Extracting the order of the stages of the end of heaven, from its first state to its last, which came in separate verses of the Qur’an, each one of which was placed in a surah that was consistent w
... Show MoreThe study of the future of the international system currently appears, according to scientific data and existing facts in light of the emergence of international actors from non-states and international informal institutions, to be heading towards a non-polarity system and this trend is fueled by many variables to reduce polarity, and it is expected in the future that the international system will turn into a non-polarity.
In this study, the effect of the thermal conductivity of phase change material (PCM) on the performance of thermal energy storage has been analyzed numerically. A horizontal concentric shell-and-tube latent heat thermal energy storage system (LHTESS) has been performed during the solidification process. Two types of paraffin wax with different melting temperatures and thermal conductivity were used as a PCM on the shell side, case1=0.265W/m.K and case2=0.311 W/m.K. Water has been used as heat transfer fluid (HTF) flow through in tube side. Ansys fluent has been used to analyze the model by taking into account phase change by the enthalpy method used to deal with phase transition. The numerical simulatio
... Show MoreThis research presents a study for precipitating phosphorus (as phosphate ion) from simulated wastewater (5ppm initial concentration of phosphorus) using calcium hydroxide Ca(OH)2 solution. The removal of phosphorus by Ca (OH)2 solution is expected to be very effective since the chemical reaction is of acid-base type but Ca(OH)2 forms complex compound with phosphate ions called. Hydroxyapatite Ca5 (PO4)3OH. hydroxyapatite is slightly soluble in water. This research was directed towards sustainable elements as phosphorus. Kinetics of the dissolution reaction of hydroxyapatite was investigated to find the best factors to recover phosphorus. The effect of con
... Show MoreNisoldipine (NSD) is a dihydropyridine class of calcium channel blockers used for hypertension treatment, it belongs to class II BCS (low solubility with high permeability), its absolute bioavailability is only 5% due to presystemic metabolism in the gut wall. It is also a substrate for a CYP3A and P-gp. Bilosomes are lipid bilayer vesicles incorporating bile salts in their walls to prevent degredation by GIT bile salts. The aim of this study is to prepare nisoldipine bilosomes as vesicular carrier and assess the effect of different formulation variables such as type of surfactant, amount of cholesterol, surfactant and sonication time on particle size, entrapment efficiency and poly dispersity index of the prepared bilos
... Show MoreBackground: Periodontal diseases are bacterial infections of the gingiva, bone and attachment fibers that support the teeth and hold them in the jaw. Lactoferrin is a multifunctional glycoprotein and it is the main component of neutrophil polymorphonuclear leukocytes that activated during inflammatory processes such as Periodontal diseases Aims of the study: Determine the salivary levels of Lactoferrin and pH and their correlations with clinical periodontal parameters(Plaque Index , Gingival Index , Bleeding on Probing , Probing Pocket Depth , and Clinical Attachment Level ) and the correlation between Lactoferrin with potential of hydrogen ion (PH) ,flow rate and α-amylase of study groups that consisted of patients had gingivitis and pa
... Show MoreG. tuberculosa is a newly recorded species from the Caryophyllaceae family for Iraqi flora, collected from the Arbil district from May to August. Morphological descriptions with macro and micro features illustrated with plates and dimensions, the species is related to G. pallida and distinguished from calyx properties, especially the presence of large prominent druses crystals. Keywords: Caryophyllaceae, Gypsophila, Iraq, New record, pallida.
The antimicrobial activity of two naphthoquinone semicarbazone derivatives (Two newly synthesized compounds) have been studied by using tube — diluation and disc plate technique. The effect of those derivatives upon pathogenic microorganism iso-lated from specimen(urine iwounds,stool, swabs, throat ....etc) have been studied also in comparison with the antibiotics (amikacin,ampicillin, carbencillin, cephalothin, cefoxitin,clindamycin ,erythromycin,gentamycin,penicillin,tetracylin and tri-methoprim. It was shown that derivative(1) had more effective against micro organ-ism than derivative(11).
Propranolol is a nonselective-adrenergic blocker used in the treatment of hypertension, cardiac arrhythmias, and angina pectoris. A significant problem in propranolol therapy is that it undergoes extensive presystemic metabolism after oral administration leading to reduced bioavailability. In this study, two new propranolol derivatives have been designed, synthesized and characterized. These compounds were formed by acylation of propranolol followed by nucleophilic substitution reaction of acylated propranolol, these derivatives were analyzed for IR, CHN, melting points, and evaluated for their lipophilic properties compared with propranolol. The lower partition coefficient of these two derivatives revealed that the prodrug approach may be
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