Synthesis and structure-activity relationships of N-substituted 2-[(2-imidazolylsulfinyl)methyl]anilines as a new class of gastric H+/K(+)-ATPase inhibitors.

A series of N-substituted 2-[(2-imidazolylsulfinyl)methyl]anilines (3) was synthesized and evaluated for its biological activity against gastric H+/K(+)-ATPase prepared from rabbit stomach and gastric acid secretions in Heidenhain pouch dogs. Monoalkyl substituents on the nitrogen atom of the aniline moiety markedly inhibited the enzyme activity to the same degree as omeprazole, a representative H+/K(+)-ATPase inhibitor. Most of these compounds, administered at 3 mg/kg i.v. inhibited histamine-stimulated gastric acid secretion. The inhibitory activity of these derivatives on the enzymes at pH 6.0 was more potent than that at pH 7.4, and was distinctly correlated to stability in aqueous solution at pH 5.0.     

Structure of norbornene-fused 3,1-oxazine double cycloadducts

Pentacyclic isoxazolines were obtained by the cycloaddition of benzonitrile oxide to norbornene-azetidinone-fused 3,1-oxazines. The constitutions of two of the isomers obtained, and the configurations and conformations of all products, were determined by means of ¹H and ¹³C NMR spectroscopy and DNOE experiments.     

An Inventory Model for Deteriorating Items and Stock-dependent Consumption Rate

An order-level inventory model is developed for deteriorating items with uniform rate of production and stock-dependent demand. Shortages are allowed, and excess demand is backlogged. Results are illustrated with numerical examples.

     

The Gaussian cotype of operators fromC(K)

We show that the canonical embeddingC(K) →L _Φ(μ) has Gaussian cotypep, where μ is a Radon probability measure onK, and Φ is an Orlicz function equivalent tot ^p(logt) ^p/2 for larget.     

Simultaneous best approximation by three polynomials

Let [a, b] be any interval and let p₀, p₁, p_k be any three polynomials of degrees 0, 1, k, respectively, where k 2. A set of necessary and sufficient conditions for the existence of an f in C[a, b] such that p_i is the best approximation to f from the space of all polynomials of degree less than or equal to i, for all i = 0, 1, k, is given.