Research
Drug Synthesis, Analysis and Characterisation
Since routinely fast in silico methods and in vitro high-throughput assays are performed for drug design, structural optimisation, and activity testing, the bottleneck of drug development often consists in their synthesis. This is reflected by the fact that in recent years, the number of synthetic pharmaceutical/medicinal chemists in industrial drug development programmes was increased. This happened for example in the search for antibacterial agents at GlaxoSmithKline (see Nature Rev. Drug Discov 2007; doi:10.1038/nrd2201 ). Synthetic robots of course enormously increases the output of test substances, but also results in low diversity of the synthetic methods. A pharmaceutical chemist from the industry summarised the problem succinctly: "It would do us (and our compound collections) good if our molecules were a little less flat, a little less aromatic, and perhaps a little less easy to put together." (www. rsc. org/chemistryworld/Issues/2008/August/ColumnInpipeline. asp )
That is why we have a go at somewhat special structures that could be drugs or diagnostic agents, and try to construct and vary them. This is an endeavor requiring a lot of creativity, skill and perseverance.
We focus on plant or microbial natural products, as well as potential human metabolites of known drugs. Metabolites are indeed more often than expected co-responsible for the molecular basis of drug effects. We are looking for molecules with special molecular features, exploring how they could be used in drug design, or how their use could be optimised. We hope to find leads providing a better understanding of molecular mechanisms of drug action. The activity of our substances is tested in cooperation with research groups that have the appropriate assays, etc. – resulting in an attractive 'side effect', viz. the opportunity to spend instructive and productive time in another university or research centre, sometimes even in another country.
We currently conduct research in the following fields: