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.
Abstract
The present investigation aimed to formulate a liquid self-microemulsifying drug delivery system (SMEDDS) of tacrolimus to enhance its oral bioavailability by improving its dispersibility and dissolution rate. Four liquid SMEDDS were prepared using maisine CC as oil phase, labrasol ALF as surfactant and transcutol HP as co-surfactant based on the solubility studies of tacrolimus in these components. The phase behavior of the components and the area of microemulsion were evaluated using pseudoternary phase diagrams. The formulations were also assessed for thermodynamic stability, robustness to dilution, self-emulsification time, drug content, globule size and polydispersity index. The prepared SMEDDS formulations exhibi
... Show MoreThe Chemistry of heterocyclic sulphur and nitrogen containing compounds have a great role in the field of scientific studies, The 2-amino 5-mercapto-1,3,4-thiadiazole ring for instance, has gained more importance in recent years because they are considered as potent biologically active nucleus. In this study disulfide derivative can be obtained by oxidation with hydrogen peroxide of thiol group of the heterocyclic 2-amino 5-mercapto-1,3,4-thiadiazole ring to obtain compound (3) with expected antibacterial activity. In order to use it as a diazo component to prepare some new bis azo compounds as possible antibacterial agents, the reaction of two primary amino groups on both sides of disulfide dimer with sodium nitr
... Show MoreOne of the major problems facing the road construction engineer is the collapsible granular soil which may be used for embankment construction. Problems appears when such compacted soil come in touch with water, it exhibits cracking and uncontrolled settlement. Collapsible soils are defined as any unsaturated soil that goes through a radical rearrangement of practice and great loss of volume upon wetting, with or without additional loading. An attempt has been made in this investigation to stabilize the collapsible soil of Nasiriya with asphalt emulsion. Specimens of pure and asphalt emulsion stabilized soil have been prepared using optimum fluid content and tested. The first group of specimens of (60x60x20) cm have been tested for direct s
... Show Morein this paper sufficient conditions of oscillation of all of nonlinear second order neutral differential eqiation and sifficient conditions for nonoscillatory soloitions to onverage to zero are obtained
Doxycycline and levofloxacin are heterocyclic organic compounds that are now popularly used to treat some bacterial infections. In this study which was conducted on patients from a private clinic, we compared the use of two commonly used antibiotics for the treatment of diagnosed cases with vaginal chlamydial infection: levofloxacin and doxycycline. Vaginal chlamydial infection is considered to be a very common sexually transmitted infection. It may have minimal symptoms which can lead to neglect by the patient until it leads to some important complications among which is the inability to become pregnant. This indicates early diagnosis and treatment of this infection. By comparing the results of treatment we concluded that there is no much
... Show MoreTwo isolates of Staphylococcus xylosus (urease producer and non urease producer) were injected in mice at a dose of 2 × 108 colony-forming units (CFU) intraurethrally. Results showed that both isolates were able to colonize kidney and bladder of the injected mice, regardless of their urease production. Moreover, there were insignificant differences between the two groups. These results emphasized the pathogenicity of this bacteria in UTI.
Background: Pregnancy is a natural physiological state that involves several biochemical modifications. Saliva is consisted of many types of proteins such as salivary alpha amylase and salivary peroxidase that might be affected by pregnancy. The former enzyme is considered one of the most prevalent proteins that is released by highly differentiated epithelial acinar cells and has been shown to have enzymatic activities while the latter has been approved that it has a significant role in oral health. The purpose of this study was to the evaluate the salivary levels of alpha-amylase and peroxidase in pregnant and non-pregnant women. Materials and Methods: Sixty pregnant women were grouped according to the pregnancy trimesters. The first
... Show MoreThe purpose of this study is to explore whether the adoption of Beyond Budgeting (BB) as a management accounting practice (MAP) contributes to developing intellectual capital (IC) and creating value in Iraqi companies. This requires an understanding of the views of the Iraqi managers about the nature of the information provided by this practice, which may be used to determine whether this information is relevant in the management of IC in the context of Iraq. This research aims also to explore the challenges of the adoption of the BB in planning and controlling IC in Iraq. The study adopts a qualitative approach and an interpretive paradigm. It also adopts a semi-structured interview method of collecting data from executive managers
... Show MoreThe recent development in statistics has made statistical distributions the focus of researchers in the process of compensating for some distribution parameters with fixed values and obtaining a new distribution, in this study, the distribution of Kumaraswamy was studied from the constant distributions of the two parameters. The characteristics of the distribution were discussed through the presentation of the probability density function (p.d.f), the cumulative distribution function (c.d.f.), the ratio of r, the reliability function and the hazard function. The parameters of the Kumaraswamy distribution were estimated using MLE, ME, LSEE by using the simulation method for different sampling sizes and using preli
... Show More