Innovative synthetic strategies giving access to a larger chemical space are of great importance to make the development of peptide therapeutics a faster and more efficient process. Katritzky salts, easily prepared from primary amines, offer peptide chemists a tool to achieve many chemical transformations in a straightforward manner.
IRBM’s drug discovery research is featured on the cover of this issue’s ACS Publications’ Medicinal Chemistry Letters
The publication describes the discovery of a novel series of Imidazopyrazine derivatives by IRBM’s drug discovery team. This novel series of SHP2 allosteric inhibitors, having an imidazopyrazine 6,5-fused heterocyclic system as central scaffold, showed an excellent potency in enzyme and cellular assays. X-ray studies confirmed novel stabilizing interactions with respect to known SHP2 inhibitors. These compounds paved the way to the discovery of preclinical candidates.
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