School 1: Modern synthetic methodologies leading to neurotrophin small molecule mimetics

During the third day of School 1, which was held at NHRF on December 7th 2018, students had the opportunity to hear more information about neurotrophin copycats from Prof. Theodora Calogeropoulou. She explained which ligands for neurotrophin receptors are discovered until now and why is the 17-spiro substituted steroidal scaffold one of the topics of the research for the Euroneurotrophin project.
Prof. Christophe Rochais held the presentation about synthetic methodologies and medicinal chemistry toolboxes. In his presentation, Prof. Rochais explained to the students some of the potential synthetic pathways for obtaining neurotrophin small molecule mimetics and the methods used for developing the good synthetic procedure. At the end of the presentation, students were divided into small groups and each group got a compound to identify its synthetic route and conditions from commercially available sources using Reaxys website. Four ERSs (Daniele Narducci, Alessia Latorrata, Paolo Giaccio and Mirjana Antonijevic) tutored each group during this exercise in order to help other students to understand each part of the synthetic procedure. Students got an insight in small part of synthetic chemistry and how complex it can be, how does the process of discovering a good synthetic route looks like and what are the new procedures in drug discovery.

At the end of the day, Prof. Calogeropoulou talked about the dynamic libraries for hit discovery. This modern approach of combining different functional groups in order to get various ligands for one target represents a potential way of drug discovery.