A new 5‐fluorouracil–naproxen conjugate is synthesized as a mutual prodrug for targeting cancer tissues. The structure of the target compound and their intermediate are characterized by their melting point, IR, 1H NMR, 13C NMR, and elemental microanalysis. The cytotoxic activity is preliminarily evaluated using nonsmall lung cancer CRL‐2049, human breast cancer CAL‐51, and one type of normal cell line; rat embryo fibroblast cell line. The synthesized compound shows a good cytotoxic effect at the cancer cell and no significant effect at rat embryo fibroblast cell line.
New heterocyclic derivatives of quinoline are reported. Reaction of quinoline-2-thiol 4 with hydrazine hydrate gave 2-hydrazionoquinoline 5. Treatment of 5 with CS2 in pyridine afforded 1,2,4-triazolo-[4,3-a]- quinolin-1-2H-thione 6, whereas the reaction of 5 with carboxylic acids namely formic acid or acetic acid, yielded the 1,2,4-triazol-[4,3-a]-quinolin 7 or 5-methyl-1,2,4-triazolo [4,3-a]-quinoline 8 through ring closure. Diazotization of 5 under acidic conditions produced the fused tetrazole compound 9, tetrzolo-[1,5-a]- quinoline. Moreover, treatment of 5 with active methlyene compounds gave two pyrazole derivatives 10 and 11. Azomethines 12a-e were prepared through condensation of 5 with aromatic aldehydes or ketones.
The discovery of novel therapeutic molecules is always difficult, and there are a variety of methodologies that use the most diverse and innovative medicinal chemistry approaches. One such approach is the deuteration technique: Deuteration is the process of substituting deuterium for hydrogen in a molecule. When compared to the drug molecule, its deuterated analogues may retain the features of the original molecule and, in some cases, improve its pharmacological activity, with fewer side effects and lower toxicity. Metronidazole is a commonly used antibiotic to treat anaerobic bacterial infections, protozoal and microaerophilic bacterial infections. Met
... Show MoreIn this research, main types of optical coatings are presented which are used as covers for solar cells, these coatings are reflect the infrared (heat) from the solar cell to increase the efficiency of the cell (because the cell’s efficiency is inversely proportional to the heat), then the theoretical and mathematical description of these optical coatings are presented, and an optical design is designed to meet this objective, its optical transmittance was calculated using (MATLAB R2008a) and (Open Filters 1.0.2) programs
This study is concerned with shedding light on the grammatical method of Ibn Hisham Al-Ansari (761 AH), in his explanation of Bant Souad’s poem by the poet Kaab bin Zuhair, and I included a brief description of Ibn Hisham’s life with a number of explanations of this poem, then clarified the most important features of this method The grammar represented by his reliance on hearing and presenting it to analogy with mention of types of analogy, as well as his attribution of opinions to their owners with weighting, selection and balancing, and his attention to reasoning and a number of grammatical ailments, and his approach is also distinguished by following the method of fractal.
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Laser shock peening (LSP) is deemed as a deep-rooted technology for stimulating compressive residual stresses below the surface of metallic elements. As a result, fatigue lifespan is improved, and the substance properties become further resistant to wear and corrosion. The LSP provides more unfailing surface treatment and a potential decrease in microstructural damage. Laser shock peening is a well-organized method measured up to the mechanical shoot peening. This kind of surface handling can be fulfilled via an intense laser pulse focused on a substantial surface in extremely shorter intervals. In this work, Hydrofluoric Acid (HF) and pure water as a coating layer were utilized as a new technique to improve the properti
... Show MoreThe current research aims to identify the effect of the learning mastery strategy using interactive learning as a therapeutic method on the achievement of secondary school students in mathematics. To achieve the research objective, the researcher selected second-grade middle school students at Al-Haybah Intermediate School for Boys and determined his research sample, which consisted of (77) students distributed into two sections: Section (A) the experimental group, with (38) students, and Section (B) the control group, with (39) students. The statistical equivalence of the two research sample groups was confirmed in the variables (intelligence test, previous achievement, and previous knowledge test). The researchers chose the par
... Show MoreExtreme conditions will cause the water level of high fill canal segment to change suddenly, which will affect the velocity and pore pressure of the slope. A 9 km irrigation earth canal in the city of Alsyahy, 15 km away from Al-Hilla city, and branching off from the left side of Shatt Al-Hilla at 57 km, was studied. The aim of this work is to study and analyze the effect of rationing system on the Birmana earthen canal during rapid drawdown case. Finite element modeling with Geo-Studio software was used in the present study to analyze the combined seepage and slope stability for three cycles. The resulting minimum safety factor obtained from the analysis using the saturated and