Asymmetric Cycloaddition: An Efficient Synthesis of Enantiopure Isoxazolines Substituted with Carbohydrate Analogues

A simple and convenient method for the synthesis of heterocycles substituted with carbohydrate analogs is described. The chiral optically pure five‐membered glycoconjugates containing the isoxazoline unit were obtained by an aromatic nitrile oxides cycloaddition with 1‐phenyl‐1,2‐dihydro‐pyridazine‐3,6‐dionyl N‐glycoside derivatives.     

New Analytical Method using Coupled Enzymes for Determination of Polyunsaturated Fatty Acid Content in Olive Oil

A new, simple, and original method is described for specific measurement of polyunsaturated fatty acid content in olive oil. This analytical system uses coupled enzymes, lipase and lipoxygenase. The system consists of lipase-catalyzed hydrolysis of triacylglycerol and subsequent lipoxygenation of liberated polyunsaturated fatty acids. The hydroperoxy-fatty acids formed were easily monitored by spectrophotometry at 234 nm. After being optimized, the method was validated in terms of linearity, precision sensitivity, and recovery. Linear calibration graph was obtained in the range 50–500 µg mL^?1, with a correlation coefficient higher than 0.921 and a detection limit (S/N?=?3) of 15 µg mL^?1. The precision of the method (relative standard deviation) for within and between days is better than 7% and 12%, respectively. The proposed method was successfully applied to the estimation of polyunsaturated fatty acids level in olive oil samples and results obtained were in excellent agreement with those obtained by the classical official method. The proposed method is accurate, simple, cheap, and can be satisfactorily used for routine analysis of edible oils.     

Transformations de N-acylaziridines catalysées par des supports à base de silice et d’alumine : une élucidation mécanistique

The silica gel, neutral alumina and acid activated clays transform the N-acyl-2,2-dimethylaziridines 1 into a mixture of N-methallylamides 2, oxazolines 3 and amidoalcohols 4. The reaction of N-benzoyl-2,2-dimethylaziridine with benzylcyanid anion leads to a mixture of amidopyrroline 5 and iminopyrrolidine 6. The product 5 was converted into its tautomer 6 by chromatogaphy on silica gel. Ionic mechanisms were then proposed to explain the formation of products 2–6 resulting from the regioselective ring opening on the more substituted C2 carbon side.     

Two Optimal General Classes of Iterative Methods with Eighth-Order

Two new three-step classes of optimal iterative methods to approximate simple roots of nonlinear equations, satisfying the Kung-Traub’s conjecture, are designed. The development of the methods and their convergence analysis are provided joint with a generalization of both processes. In order to check the goodness of the theoretical results, some concrete methods are extracted and numerical and dynamically compared with some known methods.     

On the Symmetric H q -Semiclassical Polynomial Sequences of Even Class. Some Examples from the Class Two

In the present work, we deal with the quadratic decomposition of symmetric H _q -semiclassical polynomial sequences of even class. Some examples from class two are settled. We give an integral and discrete measure representations for each of considered symmetric forms.     

Synthesis and evaluation of new phosphonated δ-lactam and glutarimide derivatives as angiotensin converting enzyme inhibitors

An efficient synthesis of new γ,δ-insaturated δ-lactam and glutarimide derivatives bearing a phosphonomethyl group from a common allylphosphonate precursor is described. Our approach is based on a two-step procedure involving the preparation of phosphonated-1,5-ketoester and −1,5-diester followed by an amidation–heterocyclization sequence. The first step proceeds via Michael's addition of ethyl acetoacetate and diethyl malonate on an allylphosphonate starting material. The second step consists of a base-promoted intramolecular amidation-cyclization sequence with primary amines, which accounts for the construction of δ-lactams and glutarimide skeletons. We performed the evaluation of angiotensin I-converting enzyme (ACE) inhibition using an in vitro enzyme assay on six new compounds. Five compounds showed potent ACE inhibitory activity, with IC₅₀ values ranging from 0.02 to 0.27 mg/ml. Compared with Captopril, used as a reference drug, two new glutarimide derivatives exhibited higher efficiency ACE inhibition activity.     

Stability indicating method for famotidine in pharmaceuticals using porous graphitic carbon column

A simple, sensitive and rapid HPLC method was developed and validated for the simultaneous determination of famotidine (FMT) and related impurities in pharmaceuticals. Chromatographic separation was accomplished within 10 min on a porous graphitic carbon (PGC) column using 50:50 v/v ACN-water containing 0.5% pentane sulphonic acid (PSA) as the mobile phase. Separation was achieved with a flow rate of 1 mL/min and a detection wavelength of 265 nm. The calibration curves were linear over a concentration range of 1.5-100 microg/mL. The intra- and interday RSDs (n = 5) for the retention times and peak area were all less than 2%. The method was sensitive with an LOD (S/N = 3) of 0.1 microg/mL for FMT, imp. C and 0.05 microg/mL for imp. 2, A and D. All recoveries were greater than 98%. The method was demonstrated to be precise, accurate and specific with no interference from the tablet ingredients and separation of the drug peak from the peaks of the degradation products (oxidative degradation and acid and base degradation). The results indicated that the proposed method could be used for the determination of FMT in commercial dosage forms and as a stability-indicating assay.     

Effect of Host Medium on the Fluorescence Emission Intensity of Rhodamine B in Liquid and Solid Phase

In this work, we study the effect of concentration, host medium, PH and phase states on the fluorescence emission from the laser dye Rhodamine B pumped by UV laser as exited source. The polymethylmethacrylate PMMA is used as a host medium in case of solid phase samples while, ethanol and Tetrahydrofuran (THF) are used in case of a liquid one. Laser Induced Fluorescence (LIF) technique was used to study the fluorescence properties of both cases of liquid and thin film solid-state samples. In addition, the Dual Thermal Lens (DTL) technique was used to study the quantum yield of these samples. The concentrations of Rhodamine B in ethanol as solvent between 2 × 10⁻² M and 5 × 10⁻⁶ M were studied. The maximum fluorescence emission is observed at concentration of Rhodamine B C = 3 × 10⁻⁴ M. Comparison studies were investigated for different host medium such as ethanol, THF, PMMA in liquid phase state and PMMA in solid phase state. The measurements revealed that, the behavior of both phases state was analogous. Rhodamine B/PMMA thin film sample by ratio of 4:1 and thickness 0.12 mm was found to have the best photostability sample with a quantum yield about ≈0.82.     

Purification and structure elucidation of three naturally bioactive molecules from the new terrestrial Streptomyces sp. TN17 strain

Thirty litres of fermentation broth was extracted from the newly isolated Streptomyces sp. strain TN17 and various separation and purification steps led to the isolation of three pure bioactive compounds (1-3). Compound 1: cyclo (L-Leu-L-Arg), a diketopiperazine 'DKP' derivative; 2: di-(2-ethylhexyl) phthalate, a phthalate derivative; and 3: cyclo 1-[2-(cyclopentanecarbonyl-3-phenyl-propionyl]-pyrrolidine-2-carboxylic acid (1-carbamoyl-propyl)-amide, a cyclic tetrapeptide derivative. The chemical structure of these three active compounds was established on the basis of spectroscopic studies (MS and NMR) and by comparison with data from the literature. According to our biological studies, the pure compounds (1-3) possess antibacterial and antifungal activities.     

Convenient synthesis of substituted benzo[e][1,2,4]- or [d][1,2,6]oxadiazepines,benzo[f][1,3,5]triazocines from N-aryliminoesters

We report herein a short and efficient synthesis of benz[e][1,2,4]- or [d][1,2,6]oxadiazepines and benzo[f][1,3,5]triazocines from easily prepared N-aryl iminoesters. The strategy involves a bis-nucleophile reagent (hydroxylamine or guanidine) that promotes a one-step ring closure from the starting functionalized iminoesters.