This research includes synthesis of new heterocyclic derivatives of N-benzyl-5-bromoisatin. New 1, 2, 4-triazole, oxazoline and thiazoline derivatives of [N-benzyl-5-bromo-3-(Ethyliminoacetate)-indole-2-one] (2) have been synthesized. The preparation process started by the reaction of 5-bromoisatin with sodium hydride in dimethylformamide (DMF) at 0°C, gave suspension of sodium salt of 5-bromoisatin and subsequent reaction with benzylchloride to give N-benzyl-5-bromoisatin (1). Compound (1) reacted with ethylglycinate (Schiff base) obtained the intermediate compound (2) which reacted with different reagents in two ways. The first way, compound (2) reacted with (hydrazine hydrate, semicarbazide, phenylsemicarbazide and thiosemicarbazide), then converted to (hydrazide, semicarbazide, phenylsemicarbazide and thiosemicarbazide) derivatives respectively to give compounds (3-6). After that compounds (4-6) cyclized in presence of alkaline media (4N-NaOH) to form substituted 1, 2, 4-triazole derivatives (7-9). In alkaline media (20%KOH) compound (3) reacted with CS2 to give potassium salt (10) that reacted with excess of hydrazine hydrate to give compound (11). The second way includes reaction of compound (3) with (phenylisocyanate and phenylisothiocyanate) to give compound (5 and 12), which undergo cyclization with p-bromophenacylbromide to obtain oxazoline (13) and thiazoline (14). Newly synthesized compounds were identified via spectral methods; their [FTIR and some of them by 1HNMR, 13C-NMR] and measurements of some of its physical properties and also some specific reactions. Furthermore the effects of the synthesized compounds were studied on some strains of bacteria.
Drug nanocrystals are nanoscopic crystals of the parent compound with dimensions less than 1 µm. A decrease in particle size will lead to an increase in effective surface area in the diffusion layer, which, in turn, increases the drug dissolution rate. Drug nanocrystals are one of the most important strategies to enhance the oral bioavailability of hydrophobic drugs.
Cefixime is the first member of what is generally termed the third generation orally active cephalosporins. These third generation cephalosporins are distinct from the older β-lactam antibiotics in their intensive antibacterial activity against a wide range of gram-negative bacteria.
The aim of this study is to prepare nanocrystals of cefixime as a caps
... Show MoreThe aim of this study is to formulate and evaluate ezetimibe nanoparticles using solvent antisolvent technology. Ezetimibe is a practically water-insoluble drug which acts as a lipid lowering drug that selectively inhibits the intestinal absorption of cholesterol and related phytosterols. Ezetimibe prepared as nano particles in order to improve its solubility and dissolution rate.
Thirty formulas were prepared and different stabilizing agents were used with different concentrations such as poly vinyl pyrrolidone (PVPK-30), poly vinyl alcohol (PVA), hydroxy propyl methyl cellulose E5 (HPMC), and poloxamer. The ratios of drug to stabilizers used to prepare the nanoparticles were 1: 2, 1:3 and 1:4.
The prepared nanoparticles
... Show MoreThe present study is to formulate and evaluate Acyclovir (ACV) microspheres using natural polymers like chitosan and sodium alginate. ACV is a DNA polymerase inhibitor used in treating herpes simplex virus infection and zoster varicella infections. Acyclovir is a suitable candidate for sustained-release (SR) administration as a result of its dosage regimen twice or thrice a day and relatively short plasma half-life (approximately 2 to 4 hours). Microspheres of ACV were prepared by an ionic dilution method using chitosan and sodium alginate as polymers. The prepared ACV microspheres were then subjected to FTIR, SEM, particle size, % yield, entrapment efficiency, in vitro dissolution studies and release kinetics mechanism. The FTI
... Show Moreاثناء تفاعل الديزنة تكونت صبغة أزو جديدة عن طريق تفاعل 3-امينوفينول مع 2,4,6-ثلاثي هيدروكسي اسيتوفينون . ثم تم تفاعل هذا الليكاند مع بعض ايونات العناصر الكروم والحديد الروديوم والروثينيوم بتكفؤهم الثلاثي والكوبلت الثنائي والموليبدينوم سداسي التكافؤ مكونة معقدات فلزية مختلفة بأشكال هندسية متعددة. تم ملاحظة تناسق مجموعة الازو مع ايونات العناصر من خلال ملاحظة ظهور حزم امتصاص الفلز مع النتروجين والاوكسجين ب
... Show MoreA total number of 68 water samples was revealed 20 isolates being Staphylococcus aureus. Irrigation water isolates represented 25% of isolates while wastewater 75%. all isolates were identified by morphological, microscopial, biochemical tests and VITEK®2 Compact. Bacterial isolates were subjected to 16 antibiotics, all irrigation water and wastewater isolates were resistant to penicillin while they were fully sensitive to Ciprofloxcin. Irrigation water isolates showed relatively greater multi-drug resistance than wastewater, wherein irrigation water isolates showed 100% multi-drug resistance while wastewater isolates showed 73.3% multi-drug resistance, indicating the ability of S. aureus MDR to move from one site to another, which means t
... Show MoreThis work aimed to use conventional PCR to identify Salmonella spp. that were isolated from diarrheal children and healthy and diarrheic dogs based on four virulence genes, hilA, stn, spvR, and marT. Sixteen Salmonella isolates including: 9 isolated from children's diarrhea from three species (S. Typhimurium, S. Enteritidis, S. Typhi) and seven isolated from dogs including (S. Typhimurium, S. Enteritidis, S. Muenchen), were identified primarily by several methods. The PCR products of the 16S rRNA gene were sequenced and examined using BLAST analysis to find differences and similarities between these Iraqi isolates and already-known global strains in order to construct the phylogenetic tree of S.
... Show MoreIn this research, a novel synthesis of CaONPs has been developed via an environmentally friendly, green method. Garlic extract (Allium sativum) was used as a green-reducing and stabilizing agent for CaONPs. The average particle size of CaONPs was approximately 24.42 nm. The synthesized CaONPs were identified by using Fourier transform infrared (FT-IR) spectroscopy, U.V.-vis spectrum, X-ray diffraction (XRD), Field Emission-Scanning Electron Microscopy (FE-SEM), Transmission Electron Microscopy, transmission electron microscopy (TEM), Energy Dispersive X-ray spectroscopy (EDX), Atomic Force Microscopy (AFM), and zeta potential (Zp) analysis. The current study highlights the notable applications for CaONPs. First, an antimicrobial assay revea
... Show MoreMixed ligand metal complexes of CrIII, FeIII,II, NiII and CuII have been synthesized using 5-chlorosalicylic acid (5-CSA) as a primary ligand and L-Valine (L-Val) as secondary ligand. The metal complexes have been characterized by elemental analysis, electrical conductance, magnetic susceptibility measurements and spectral studies. The electrical conductance studies of the complexes indicate their electrolytic nature. Magnetic susceptibility measurements revealed paramagnetic nature of the all complexes. Bonding
In a connected graph , the distance function between each pair of two vertices from a set vertex is the shortest distance between them and the vertex degree denoted by is the number of edges which are incident to the vertex The Schultz and modified Schultz polynomials of are have defined as:
respectively, where the summations are taken over all unordered pairs of distinct vertices in and is the distance between and in The general forms of Schultz and modified Schultz polynomials shall be found and indices of the edge – identification chain and ring – square graphs in the present work.
Aromatic Schiff-bases are known to have antibacterial activity, but most of these compounds are sparingly soluble in water. The present work describes the synthesis of new Schiff-bases derived from branched aminosugars. Treatment of 3-Amino-3-Cyano-3-Deoxy-1,2:5,6-Di-O-Isopropylene-α-D-Allofuranose (1) with the aldehydes (2) under reflux in methanol afforded the Schiff-bases (3) in good yields. The new Schiff-bases were in accord with their NMR, IR spectral data and elemental analysis.