Grant: Engage Plus Grants Program

Over the past decade, there has been a substantial reshaping of the drug-discovery model throughout thepharmaceutical industry with the objective of overcoming a drop in productivity. As part of this remodeling,companies have seeked collaborations with scientists from academic environments in order to identify newbiological targets, to diversify their compound collections or to design more efficient synthetic processes toaccess bioactive compounds. Paraza Pharma is a company that is involved in drug discovery of early clinicalcandidates. Currently, Paraza Pharma Inc. does not possess its own proprietary compound collection to conductscreening campaigns and must therefore rely on commercial libraries. However, these libraries are alsoavailable worldwide to competitors, thus reducing the competitiveness of Paraza Pharma Inc.. In addition, thesecollections of molecules often show low structural diversity and are sometimes populated with a significantnumber of compounds with poor chemical or biophysical properties. Our group has reported a portfolio ofefficient methods that allow the installation of aromatic fragments on privileged scaffolds. With the help of anNSERC Engage grant, we developed over the past six months a method to install functionalized aryl groups onamino-alcohols, a scaffold of interest to Paraza Pharma Inc.. The goal of this NSERC Engage-Plus project willbe to apply this protocol to the arylation of a known drug molecule that possess an amino alcohol in order togenerate a small library of compounds where the biological activity is retained and where the biophysicalproperties of the arylated derivatives are modulated by the nature of the aryl fragment. This project willcontribute to the training of two graduate students from our group and will provide an expertise in reactiondevelopment to Paraza Pharma that will help them diversify their compound collection, thus increasing theircompetitivity in the pharmaceutical landscape.