Fsp3: A new parameter for drug-likeness

Abstract

The drug-likeness of a compound is a key factor during the initial phases of drug discovery. It can be defined as the similarity between compounds and drugs. Here, we collate research related to the fraction of sp³ carbon atoms (Fsp³), including related high-throughput screening (HTS) cases, structural modifications based on Fsp³, and strategies to improve it. We also introduce new synthetic methods for spirocyclic scaffolds. It is likely that the reasonable rigidity of spirocyclic scaffolds will provide a new generation of drug candidates.