Reducing of ethyl 4-((2-hydroxy-3-methoxybenzylidene)amino)benzoate (1) afford ethyl 4-((2-hydroxy-3-methoxybenzyl) amino)benzoate (2). Reaction of this compound with Vilsmeier reagent affords novel 2-chloro-[1,3] benzoxazine ring (3). The corresponding acid hydrazide of compound 3 was synthesized from reaction of compound (3) with hydrazine hydrate. Newly series of hydrazones(5a–i) were synthesized from reaction of acid hydrazide with various aryl aldehydes. Antibacterial activity of the hydrazones wassecerned utilizing gram-negative and gram-positive bacteria. Compound (5b) and (5c) exhibited significant antibacterial ability against both gram-negative and gram-positive bacteria, while the compounds(5a) showed mild antibacterial activity. Compounds (5d–i) did not display notable activity. The molecular docking of synthesised compounds were tested inside the pocket of bacterial gyrase enzyme target site by using MOE 2015 software, which acts as Adenosine triphosphate (ATP)-binding domain bacterial gyrase enzyme pocket and novobiocin was used as reference.
On the basis of known coumarin-based prodrug system, a novel coumarin-based mutual prodrug of 5-fluorouracil and dichloroacetic acid was designed, synthesized and evaluated as a promising oral chemotherapeutic agent basing on in vitro stability study in HCl buffer (pH 1.2) and in phosphate buffer (pH 7.4), as well as in vitro release study in human serum. The chemical structure of prodrug was confirmed by analyzing its FTIR, 1H NMR, 13C NMR and MS-ESI spectra. The results of in vitro kinetic study indicated that the prodrug was significantly stable in HCl and in phosphate buffers, and was hydrolyzed in human serum followed pseudo first order kinetics.
Keywords: Coumarin-bas
... Show MoreWe described herein the synthesized and characterized of new bent and liner core compounds containing thiazolidin-4-one ring[XI-XIII] and [XIV-XVI] respectively. These compounds synthesized by sequence reactions starting from reaction resorcinol or hydroquinone with chloracetyl chloride to yield compounds [I] and [II] ,then the later compounds reactant with 4-hydroxybenzylaldehyde to product dialdehyde compounds [III] and [IV] .The Schiff bases compounds[V-VII] and [VIII-X] synthesized from reaction the compound [III] or [IV] with different aromatic amines, while the bent and liner core mesogens containing thiazolidin-4-one ring [XI-XIII] and [XIV-XVI] synthesized from reaction Schiff bases compounds[V-VII] or [VIII-X] with thioglycolic aci
... Show MoreModern French novel has gained a distinctive status in the history of French literature during the first half of the twentieth century. This is due to many factors including the new literary descriptive objective style adopted by novelists like Alain Robbe – Grillet that has long been regarded as the outstanding writer of the nouveau roman, as well as its major spokesman, a representative writer and a leading theoretician of the new novel that has broken the classical rules of the one hero and evolved, through questioning the relationship of man and the world and reevaluating the limits of contemporary fiction , into creating a new form of narrative.
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... Show MoreThe aim of this study is to investigate the kinetics of copper removal from aqueous solutions using an electromembrane extraction (EME) system. To achieve this, a unique electrochemical cell design was adopted comprising two glass chambers, a supported liquid membrane (SLM), a graphite anode, and a stainless-steel cathode. The SLM consisted of a polypropylene flat membrane infused with 1-octanol as a solvent and bis(2-ethylhexyl) phosphate (DEHP) as a carrier. The impact of various factors on the kinetics constant rate was outlined, including the applied voltage, initial pH of the donor phase solution, and initial copper concentration. The results demonstrated a significant influence of the applied voltage on enhancing the rate of c
... Show MoreIntroduction The Hybrid Gamma Camera (HGC) is being developed to enhance the localisation of radiopharmaceutical uptake in targeted tissues during surgical procedures such as sentinel lymph node (SLN) biopsy. Purpose To assess the capability of the HGC, a lymph-node-contrast (LNC) phantom was constructed for an evaluative study simulating medical scenarios of varying radioactivity concentration and SLN size. Materials and methods The phantom was constructed using two methyl methacrylate PMMA plates (8 mm thick). The SLNs were simulated by drilling circular wells of diameters ranging between 10 mm and 2.5 mm (16 wells in total) in one plate. These simulated SLNs were placed underneath scattering material with thicknesses ranging between 5 mm
... Show MoreMedicine is one of the fields where the advancement of computer science is making significant progress. Some diseases require an immediate diagnosis in order to improve patient outcomes. The usage of computers in medicine improves precision and accelerates data processing and diagnosis. In order to categorize biological images, hybrid machine learning, a combination of various deep learning approaches, was utilized, and a meta-heuristic algorithm was provided in this research. In addition, two different medical datasets were introduced, one covering the magnetic resonance imaging (MRI) of brain tumors and the other dealing with chest X-rays (CXRs) of COVID-19. These datasets were introduced to the combination network that contained deep lea
... Show MoreABSTRACT The antibacterial and antbiofilm activities of water extract of Calendula officinalis flowers against some of enteropathogenic bacteria was studied, also phytochemical screening and determination of antioxidant activity of the extract has been investigated. The results showed that the water extract of C. officinalis exhibited a good antibacterial activity against all pathogenic bacterial isolates (Salmonella, Shigella dysenteriae, Shigella flexneri, Shigella sonnei and E. coli) especially at concentration 100 µg/ml in contrast with the control cefotan antibiotic. S. sonnei was more sensitive to extract than other bacteria with highest inhibition zone (23 mm). The preliminary phytochemical tests results indicated the presence
... Show MoreIn this work we used the environmentally friendly method to prepared ZrO2 nanoparticles utilizing the extract of Thyms plant In basic medium and at pH 12, the ZrO2 NPs was characterized by different techniques such as FTIR, ultraviolet visible, Atomic force microscope, Scanning Electron Microscopy, X-ray diffraction and Energy dispersive X-ray. The average crystalline size was calculated using the Debye Scherres equation in value 7.65 nm. Atomic force microscope results showed the size values for ZrO2 NPs were 45.11nm, and there are several distortions due to the presence of some large sizes. Atomic force microscope results showed the typical size values for ZrO2 NPs were 45.11 nm, and there are several distortions due to the presence of so
... Show More12 membered Schiff base macrocyclic ligands, 6,7,14,15-tetra phenyl-1,2,3,4, 4a,8a, 9,10, 11,12, 12a,16a-dodecahydro dibenzo [b,h] [1,4,7,10] tetraazacyclododecine L1, and 14 membered Schiff base macrocyclic ligands, 6,8,15,17-tetramethyl-1,2,3,4, 4a,7,9a, 10,11,12,13,13a,16,18a-tetra decahydro dibenzo[b,i] [1, 4,8,11] cyclotetradecine tetraaza L2, 7,16-bis(2,4- dichloro benz ylidene)-6,8,15,17-tetra methyl-1,2,3,4, 4a,7,9a, 10, 11,12, 13, 13a,16,18a-tetra deca hydro dibenzo [b,i] [1,4,8,11] tetra azacyclo tetra decine L3 and 6,8,15, 17-tetramethyl-1,2,3, 4,4a,9a,10, 11,12,13,13a,18a-dodecahydro dibenzo [b,i] [1,4,8, 11] tetraazacyclo tetradecine (7,16-diylidene) bis(methanylyli dene) bis (N,N-dimethylaniline) L4 were synthesized by condens
... Show MoreA new set of metal complexes by the general formula [M(P)2(H2O)2]Cl2 has been prepared through the interaction of the new Ligand [N1, N4-bis(4-methoxyphenyl)succinamide] (P) derived from succinyl chloride with p-anisidine with the transition metal ions [Cu(II), Mn(II), Cd(II), Co(II) and Ni(II)]. Compounds diagnosed by TGA, 1 H, 13CNMR and Mass spectra (for (P)), Fourier-transform infrared and Electronic spectrum, Magnetic measurement, molar conduct, (%M, %C, %H, %N). These measurements indicate that (P) is associated with the metal ion in a bi-dentate fashion by nitrogen atoms (the amide group), and the octahedral composition of these complexes is suggested. Staphylococcus Aureus (+) and Escherichia Coli (–) were studied for the antibact
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