New pyrazolone derivatives structurally related to celecoxib and FPL 62064 were synthesized and biologically evaluated for their inhibitory activity against cyclooxygenases (COXs) and 5‐lipoxygenase (5‐LOX) and their selectivity indices were calculated. The results showed that compounds 3f, 3h, 3l, and 3p have an excellent COX‐2 selectivity index. Moreover, they showed potent 5‐LOX inhibitory activity relative to celecoxib and zileuton, as positive controls. These promising candidates were further investigated for anti‐inflammatory activity using the carrageenan‐induced rat paw edema method and ulcerogenic liability. The results showed no ulceration, which implies their gastric safety profile. Moreover, these compounds were evaluated for prostaglandin (PGE2) production in rat serum. Molecular docking in the COX‐2 and 5‐LOX active sites was performed to rationalize their anti‐inflammatory activities. Strong binding interactions and effective docking scores were identified. The results indicated that these derivatives are good leads for dual‐acting COX‐2/5‐LOX inhibitors to be used as potent and safe anti‐inflammatory agents.
In this study, the phytochemical and nutritional valueofthe different parts of Bottle gourd; Lagenaria siceraria LS, cultivated in Egypt has been evaluated. Particularly, extracts of fresh/dried fruits, fresh/roasted seeds, and fresh/dried leaves of Bottle gourd were studied. Analysis of minerals, amino acids, fatty acids, phenolic compounds, flavonoids, and isoflavonoids was investigated together with the GC-MS tentative visualization of the unpolar compounds in fruits, seeds, and leaves, establishing their unique constituents. According to this study, the bottle gourd parts were confirmed to contain eleven minerals, seventeen amino acids, twenty-one phenolic analogs, ten flavonoids and four isoflavonoids. Moreover, the fresh/roasted seeds are rich with seventeen fatty acids where linoleic acid (C18:2 6) was the most abundant among them. Based on GC-MS analysis, it has been recognized that dry fruits extract revealed the presence of thirty compounds, meanwhile the fresh seeds indicated the presence of eighteen compounds, while roasted seeds hexane soluble fraction exhibited the existence of sixteen compounds and the dichloromethane soluble fraction of roasted seeds revealed the presence of ten compounds, and finally, the air-dried leaves revealed the presence of fourteen compounds.
New nonclassical acridines, quinolines, and quinazolines were prepared starting from cyclic β-diketones, namely dimedone, through application of Hantzsch addition, Michael addition, and Mannich reactions, respectively. The antimicrobial activity revealed that decahydroacridin-1,8-dione 2e bearing a 3-nitrophenyl group and hexahydroquinoline 4e having a 2,4-dichlorophenyl moiety were the most active compounds against both Gram-positive and -negative bacteria based upon using the disc diffusion method. Cytotoxic activity studies for decahydroacridin-1,8-diones 2a-e against liver carcinoma cells (HepG(2)) using the MTT cell viability assay revealed that decahydroacridin-1,8-dione bearing a 4-methylphenyl moiety 2d showed a higher cytotoxic activity (IC(50) = 4.42 µg/mL) than the other derivatives.
ZADCO's new field development program calls for drilling extended reach wells from artificial islands with the borehole kicking off at shallow depths and holding high inclination angles through the overburden. Previously, the development plan relied entirely on short reach, horizontal development wells drilled from jackup rigs with shallow overburden borehole sail angles rarely exceeding 30°. For both types of wells, bentonite weighted sea water is the preferred drilling fluid for the 16″ or 17.5″ diameter holes. Drilling problems that were managed in low-inclination wells became exacerbated at higher angles causing significant rig non-productive time (NPT). To improve our understanding of the shallow overburden formations, a comprehensive logging program was conducted in a key well drilled with a potassium chloride (KCl) mud system. Wireline borehole image, dipole shear sonic, spectroscopy and neutron-density-resistivity triple-combo logs were used to characterize the formations.
A successful logging program relies on maintaining the borehole in good condition. In this case, the KCl mud in conjunction with good drilling practices kept the hole near the 16″ bit gauge for 90% of the interval. Drilling mud losses were also minimized. The logging tools were successfully run to T.D. and the data acquired. The mineralogy of the penetrated formations was accurately quantified using spectroscopy tools. A high-resolution resistivity image log revealed that the entire interval was weakly fractured with a few zones of high secondary porosity and conductivity. These zones correlated well with zones of similar characteristics in offset wells. The key to drilling a high angle well lies is the geomechanical / geochemical characterization of the overburden formations to determine the wellbore failure mechanism(s).
This paper highlights the benefits of a KCl mud in the top hole and the results of advanced logging covering the predominately shallow carbonate formations that exist above a large carbonate reservoir. It emphasizes the need for characterizing not only the reservoir but the overburden formations. This advances drilling engineers’ understanding of formation characteristics so that increased drilling sail angles could be achieved through the shallow overburden and thus successfully reach the reservoir targets.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.