Straightforward Bienaymé and copper catalyzed N-arylation sequence to access diverse 5H-pyrido[2′,1′:2,3]imidazo[4,5-b]indoles and analogues

A two-step sequence is reported giving access to diverse 5H-pyrido[2′,1′:2,3]imidazo[4,5-b]indoles and analogues via a Bienaymé multicomponent reaction followed by N-arylation. The desired polycylic scaffolds were obtained in high yield using copper iodide in association with TMEDA in aqueous or dioxane media.     

Influence of higher interpolation orders in mixed LSFEM for the incompressible Navier-Stokes equations

The focus of this contribution is the examination of the influence of different interpolation orders (especially for the pressure field) by solving the stationary incompressible Navier-Stokes equations with least-squares finite elements. We consider two different div-grad first-order systems which result in a three-field formulation with stresses, velocitites and pressure, see e.g. SCHWARZ & SCHRÖDER [1] and BOCHEV & GUNZBURGER [2]. Additionally, a numerical example is presented to show the performance of the considered formulations. (© 2013 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim)     

Sufficient Conditions for Error Bounds and Applications

Our aim in this paper is to present sufficient conditions for error bounds in terms of Fréchet and limiting Fréchet subdifferentials in general Banach spaces. This allows us to develop sufficient conditions in terms of the approximate subdifferential for systems of the form (x, y) C × D, g(x, y, u) = 0, where g takes values in an infinite-dimensional space and u plays the role of a parameter. This symmetric structure offers us the choice of imposing conditions either on C or D. We use these results to prove the nonemptiness and weak-star compactness of Fritz–John and Karush–Kuhn–Tucker multiplier sets, to establish the Lipschitz continuity of the value function and to compute its subdifferential and finally to obtain results on local controllability in control problems of nonconvex unbounded differential inclusions.     

On the Discretization of Truncated Integro-Differential Sweeping Process and Optimal Control

Journal of Optimization Theory and Applications - We consider the Volterra integro-differential equation with a time-dependent prox-regular constraint that changes in an absolutely continuous way...     

Evaluation of N‐hydroxymethylphthalimide in alkaline medium: Novel entry to the tricyclic [1,3]oxazepine core via an intramolecular π and O‐cationic cyclization

Fused isoindolo[1,3]benzo(or thieno)oxazepines 8a,b and one of their positional isomers aromatic tricyclic N,O‐acetals 13b are reported to occur efficiently in a three‐step sequence from N‐hydroxy‐methylphthalimide (6) . The key step of this methodology is the intramolecular arylation of an endocyclic and/or exocyclic N‐acyliminium cation. The mechanism leading to these species, in particular to a tricyclic lactam 13b , is discussed.     

Diastereoselective access to chiral non‐racemic [1,3]oxazolo‐[2,3‐a]isoindol‐5‐one ring systems viaO‐cationic cyclization

Dedicated to Professor Jean Morel for his retirement The title compounds 4 have been prepared from suitable β‐amino‐ alcohol 2 and phthalic anhydride ( 5 ) in a three‐step sequence in moderate to good yields (58‐94%). The key step of this methodology is based on an intramolecular O‐cationic cyclization involving N‐acyliminium species. The high levels of the observed chemoselectivity during the intermolecular or intramolecular cyclization were also discussed.     

Theoretical investigation of the weakly dihydrogen bonded dimers H2 − nXnAlHHArF and H2 − nXnAlHHKrF (n = 0–2; X = F, Cl)

An ab initio computational study of the properties of the dihydrogen-bonded complexes of H_{2 − n}X_nAlH (n = 0–2; X = F, Cl) with the rare gas (Rg) compounds HArF and HKrF was carried out at the MP2(full)/6-311++G(2d,2p) level of theory. For all the studied complexes, we found a low zero-point corrected binding energies. Large red shifts of the H–Rg vibrational stretching frequency in both complexes were predicted. Electrostatic interactions between the individual monomers are also predicted.     

Opuntia dillenii (Ker Gawl.) Haw., Seeds Oil Antidiabetic Potential Using In Vivo,In Vitro,In Situ,and Ex Vivo Approaches to Reveal Its Underlying Mechanism of Action

Opuntia dillenii Ker Gawl. is one of the medicinal plants used for the prevention and treatment of diabetes mellitus (DM) in Morocco. This study aims to investigate the antihyperglycemic effect of Opuntia dillenii seed oil (ODSO), its mechanism of action, and any hypoglycemic risk and toxic effects. The antihyperglycemic effect was assessed using the OGTT test in normal and streptozotocin (STZ)-diabetic rats. The mechanisms of action were explored by studying the effect of ODSO on the intestinal absorption of d-glucose using the intestinal in situ single-pass perfusion technique. An Ussing chamber was used to explore the effects of ODSO on intestinal sodium-glucose cotransporter 1 (SGLT1). Additionally, ODSO’s effect on carbohydrate degrading enzymes, pancreatic α-amylase, and intestinal α-glucosidase was evaluated in vitro and in vivo using STZ-diabetic rats. The acute toxicity test on mice was performed, along with a single-dose hypoglycemic effect test. The results showed that ODSO significantly attenuated the postprandial hyperglycemia in normal and STZ-diabetic rats. Indeed, ODSO significantly decreased the intestinal d-glucose absorption in situ. The ex vivo test (Ussing chamber) showed that the ODSO significantly blocks the SGLT1 (IC₅₀ = 60.24 µg/mL). Moreover, ODSO indu\ced a significant inhibition of intestinal α-glucosidase (IC₅₀ = 278 ± 0.01 µg/mL) and pancreatic α-amylase (IC₅₀ = 0.81 ± 0.09 mg/mL) in vitro. A significant decrease of postprandial hyperglycemia was observed in sucrose/starch-loaded normal and STZ-diabetic ODSO-treated rats. On the other hand, ODSO had no risk of hypoglycemia on the basal glucose levels in normal rats. Therefore, no toxic effect was observed in ODSO-treated mice up to 7 mL/kg. The results of this study suggest that ODSO could be suitable as an antidiabetic functional food.