The Medicinal Chemistry group focuses on the design and synthesis of new compounds, the creation of molecule libraries, and collections of building blocks. The aim of the group is the discovery of new chemotypes with potential biological activity (hits) towards therapeutic targets of interest. The skills and expertise include the design, organic chemistry, and structural characterization of newly synthesized compounds, as well as the planning, development, and optimization of new synthetic routes and scale-up processes. More general and multidisciplinary skills concern cell biology, pharmacology, and toxicology. Structure-activity relationships (SAR) studies allow, through chemical manipulations, the exploration of the chemical space of biologically interesting compounds and help to better define the pharmacokinetic profile in terms of potency and efficacy. This is essential for identifying new lead compounds that are actually introduced into the pre-clinical development phase (hit-to-lead). Within the multidisciplinary context of Ri.MED Foundation Drug Discovery area, the group supports screening programs, with the following activities:

1. confirmation of the structures of preliminary actives (quality control of commercial batches),
2. synthesis of preliminary actives where necessary,
3. expansion of the chemical series of the most interesting hits during the earlier stages.

In later stages, the platform works on the structural optimization of the most promising compounds and SAR exploration for the identification of one or more potential lead compounds.

Objectives

• Discovery of new active ingredients
• Innovative chemical therapies

Focus

• Hit identification
• Hit confirmation
• Hit expansion
• Structure-activity relationship studies
• Pharmacokinetic profile optimization (hit-to-lead)

Skills and Expertise

• Pharmaceutical and organic chemistry
• Drug discovery campaigns
• Small molecules, peptides, and peptidomimetics chemistry
• Synthesis in solution, on solid support, in parallel, microwave-assisted
• Synthetic routes planning, development, optimization and scale-up
• Purification of complex mixture (normal and reverse phase)
• Isolation of compounds of interest
• Analytical characterization of newly synthesized molecules (NMR and mass spectrometry)
• Purity grade assessment

Team