Self-assembly of organic molecules with functional properties is an active area of research, aimed at creating novel materials with potential applications in nanosciences and nanotechnology. The functionalities of such materials are significantly dependent on the supramolecular organization of the molecules and morphology of the resulting nanostructures. Through the control and modulation of mo...

Despite concerns that it would be extremely difficult to design specific ATP competitive inhibitors of kinases, there have been a number of success stories including the p38 Map kinase, tyrosine kinases, and cyclin-dependent kinases.1,3 Selective inhibitors of each of these kinases are in various stages of clinical testing. The ability to discriminate between extremely homologous kinases such a...

This thesis presents a selection of the scientific activity gained by the candidate over the course of the last 14 years, including exclusively scientific results obtained after the public defence of her PhD thesis, as well as the brief description of some maine future research directions. The abilitation thesis contains 5 chapters. After the first introduction chapter, in the second (Enantioto...

Syntheses of (1RS,2SR,6SR)-2-alkoxymethyl-, 2-hetaryl-, and 2-(hetarylmethyl)-7-arylmethyl-4,7-diaza-9-oxabicyclo[4.3.0]nonan-8-ones, of interest as potential muscarinic M1 receptor agonists, are described. A key step in the synthesis of (1RS,2SR,6SR)-7-benzyl-6-cyclobutyl-2-methoxymethyl-4,7-diaza-9-oxabicyclo[4.3.0]nonan-8-one, was the addition of isopropenylmagnesium bromide to 2-benzyloxyca...

The blood-brain barrier prevents the entry of many therapeutic agents into the brain. Various nanocarriers have been developed to help agents to cross this barrier, but they all have limitations, with regard to tissue-selectivity and their ability to cross the endothelium. This study investigated the potential for 4 nm coated gold nanoparticles to act as selective carriers across human brain en...

Forming nanostructures with controlled size and shape is one of the most challenging tasks in material science. Amphiphilic block copolymers are of special interest because of their ability to self-assemble on the nanoscale. The formation of micelles has potential applications such as in drug delivery, biosensors, and gene therapy. Ring-opening metathesis polymerization (ROMP) is a versatile te...

A major effort in modern bio-organic chemistry focuses on the design, synthesis and structural characterisation of foldamers: non-natural oligomers that adopt well-defined secondary, tertiary and quaternary structures. One ultimate objective of such studies is to recapitulate the functional behaviour of biomacromolecules. Particular emphasis has been placed on inhibitors of a-helix-mediated pro...

The rate of transport of blood glutamic acid into the brain and the rate of metabolic conversion of the amino acid in the brain were derived by the use of the brain perfution method in vivo and in situ with [D.HC] ·Lglutamic acid. The net uptake of glutamic acid by the brain was observed. Most of the radioactivity released from the brain into the cerebral venous blood was found to consist of gl...

Fully protected pyrazolidines can be readily obtained by acid-catalysed cyclisations of the corresponding allylic hydrazines by carbenium ion generation using concentrated sulfuric acid in dichloromethane. Pyrazoles and their partly and fully reduced derivatives, pyrazo-lines and pyrazolidines, form an important group of heterocycles, with potentially important contributions to make to drug des...

Given the fact that the theoretically possible number of racemates is larger than that of symmetric prochiral or meso compounds, the development of deracemization methods, which yield a single stereoisomer from a racemate is an important topic. Enantioconvergent processes are based on the transformation of a pair of enantiomers through opposite stereochemical pathways affecting retention and in...