Response Surface Modelling Nafion-117 Sorption of Tetraammineplatinum(II) Chloride in the Electroless Plating of IPMCs.

This work looks at the effects of a varying concentration, soak time, pH and temperature on the sorption of tetraammineplatinum(II) chloride (Pt-Ammine) in Nafion-117 films in the context of the electroless plating of ionic polymer-metal composites (IPMCs). Sorption is characterised by atomic absorption spectroscopy. A definitive screening design carried out determined all four factors to be significant for further analysis using response surface modelling.

Isosorbide-based cholinesterase inhibitors; replacement of 5-ester groups leading to increased stability.

Isosorbide-2-carbamate-5-esters are highly potent and selective butyrylcholinesterase inhibitors with potential utility in the treatment of Alzheimer's Disease (AD). They are stable in human plasma but in mouse plasma they undergo hydrolysis at the 5-ester group potentially attenuating in vivo potency. In this paper we explore the role of the 5-position in modulating potency.

Isosorbide-2-benzyl carbamate-5-salicylate, a peripheral anionic site binding subnanomolar selective butyrylcholinesterase inhibitor.

Isosorbide-2-benzyl carbamate-5-benzoate is a highly potent and selective BuChE inhibitor. Meanwhile, isosorbide-2-aspirinate-5-salicylate is a highly effective aspirin prodrug that relies on the salicylate portion to interact productively with human BuChE. By integrating the salicylate group into the carbamate design, we have produced isosorbide-2-benzyl carbamate-5-salicylate, an inhibitor of high potency (150 pM) and selectivity for human BuChE over AChE (666000) and CES2 (23000).

Isosorbide-2-carbamate esters: potent and selective butyrylcholinesterase inhibitors.

In this study, we report the SAR and characterization of two groups of isosorbide-based cholinesterase inhibitors. The first was based directly on the clinically used nitrate isosorbide mononitrate (ISMN) retention of the 5-nitrate group and introduction of a series of 2-carbamate functionalities. The compounds proved to be potent and selective inhibitors of human plasma butyrylcholinesterase ( huBuChE).

Novel isosorbide di-ester compounds as inhibitors of acetylcholinesterase.

We report herein that a variety of isosorbide di-esters, previously reported to be novel substrates for butyrylcholinesterase (BuChE, EC 3.1.1.

Synthesis and structure activity relationships (SAR) of a new class of potent and selective butyrylcholinesterase inhibitors.

Reported here is the synthesis and SAR of novel group of highly potent and selective inhibitors of human plasma butyrylcholinesterase (BuChE; EC 3.1.1.