Chemistry of Phosphorus Ylides. Part 22 [1]. Effect of Newly Synthesized Niclosamide Mannich Bases, Phosphopyranones, Phosphoranylidenes, and Oxaphosphinin on Some Metabolic Aspects of Biomphalaria Alexandrina

Niclosamide reacts with secondary amines and formaldehyde under the condition of Mannich reaction, to give new Mannich bases. The reaction of these niclosamide Mannich bases with active phosphacumulene ylides affords the corresponding phenyliminopyranone, pyranone, and pyranthione, respectively. When Wittig reaction was carried out on the pyranone, using p-nitrobenzaldehyde, a new arylidene and triphenylphosphine oxide were obtained. On the other hand, stabilized phosphonium ylides affect the transylidation of niclosamide Mannich bases to the corresponding phosphoranylidenes. When diphenylmethylenetriphenylphosphorane reacts with a niclosamide Mannich base, an oxaphosphinin was obtained. The molluscicidal potency of the newly synthesized derivatives against Biomphalaria alexandrina was studied, too.     

1H MRS detection of glycine residue of reduced glutathione in vivo

Glutathione (GSH) is a powerful antioxidant found inside different kinds of cells, including those of the central nervous system. Detection of GSH in the human brain using ¹H MR spectroscopy is hindered by low concentration and spectral overlap with other metabolites. Previous MRS methods focused mainly on the detection of the cysteine residue (GSH-Cys) via editing schemes. This study focuses on the detection of the glycine residue (GSH-Gly), which is overlapped by glutamate and glutamine (Glx) under physiological pH and temperature. The first goal of the study was to obtain the spectral parameters for characterization of the GSH-Gly signal under physiological conditions. The second goal was to investigate a new method of separating GSH-Gly from Glx in vivo. The characterization of the signal was carried out by utilization of numerical simulations as well as experiments over a wide range of magnetic fields (4.0–14 T). The proposed separation scheme utilizes J-difference editing to quantify the Glx contribution to separate it from the GSH-Gly signal. The presented method retains 100% of the GSH-Gly signal. The overall increase in signal to noise ratio of the targeted resonance is calculated to yield a significant SNR improvement compared to previously used methods that target GSH-Cys residue. This allows shorter acquisition times for in vivo human clinical studies.     

Chemistry of Phosphorus Ylides. Part 34 Synthesis of Chromenone Phosphanylidene and Cyclobutylidene Derivatives

Abstract

The reaction of nucleophilic phosphacumulene ylides with visnaginone and khellinone afforded the corresponding phosphanylidene and furochromene derivatives. Moreover, pyranochromenes were obtained from the reaction of chromene carbaldehydes with phosphacumulenes. On the other hand, the phosphanylidene-cyclobutylidenes and their dimers were produced from the reaction of furochromene carbaldehydes with the same phosphonium reagents.     

Short TE in vivo (1)H MR spectroscopic imaging at 1.5 T: acquisition and automated spectral analysis

Spectral analysis of short TE in vivo proton magnetic resonance spectroscopic imaging (MRSI) data are complicated by the presence of spectral overlap, low signal to noise and uncharacterized signal contributions. In this study, it is shown that an automated data analysis method can be used to generate metabolite images from MRSI data obtained from human brain at TE = 25 ms and 1.5 T when optimized pulse sequences and a priori metabolite knowledge are used. The analysis approach made use of computer simulation methods to obtain a priori spectral information of the metabolites of interest and utilized a combination of parametric spectral modeling and non-parametric signal characterization for baseline fitting. This approach was applied to data from optimized PRESS-SI and multi-slice spin-echo SI acquisitions, for which sample spectra and metabolite images are shown.     

Some Isoperimetric Inequalities in Electrochemistry and Hele Shaw Flows

Isoperimetric inequalities are applied to a moving-boundaryproblem for doubly-connected domains. This problem occurs forexample in electrochemistry, in which case the domains in questionare the electrolyte of an electrolytic cell. The two electrodessurrounding the electrolyte are assumed to grow or dissolve,at different rates in general, by electrochemical reaction.We obtain optimal estimates showing, for example, that the leastchange in volume of each electrode always occurs in sphericalsymmetry.     

Chemistry of Phosphorus Ylides. Part 37. The Reaction of Phosphonium Ylides with Indoles and Naphthofurans. Synthesis of Phosphanylidenes,Pyrans, Cyclobutenes,and Pyridazine as Antitumor Agents

The reaction of the stabilized phosphonium ylides 2a , 2b with indolinones 1a , 1b and naphthofuranone 13 afforded the corresponding propylidene and ethylidene derivatives 4a , 4b , 4c , 4d and 14a , 14b . On the other hand, the active phosphacumulenes 5a , 5b react with compounds 4a , 4b , 4c , 4d by [4 + 2]‐cycloaddition to give the stable phosphanylidene indole pyranones 6a , 6b , 6c , 6d , 6e , 6f , 6g , 6h . Although compounds 14a , 14b afforded the naphthofuropyrans 16a , 16b , 16c , 16d and triphenylphosphane. Moreover, the phosphallene ylide 7 react with compounds 4a , 4b , 4c , 4d and 14a , 14b to give phosphanylidenecyclobuteneindoline 9a , 9b , 9c , 9d and naphthalenones 18a , 18b , respectively. In addition, the naphthofuropyridazine 21 was obtained from the reaction of the hydrazone 19 and the phosphacumulene 5a . The antitumor activity of some of the new compounds was evaluated, in vitro, against colon and hepatocellular carcinoma cell lines. They showed values closed to that recorded by the reference drug Doxorubicin.