ABSTRACT

Indazole is important in at least three major areas in medicinal chemistry. (a) Indazole is a good bioisostere of phenol. Generally speaking, phenol’s heterocyclic bioisosteres, including indazole, tend to be more lipophilic and less vulnerable to phase I and II metabolisms in comparison to phenol itself. (b) Indazole is a privileged fragment in FBDD. (c) Indazole has been proven to be a privileged scaffold in scaffold hopping exercises, especially for protein kinase inhibitors.