A survey of applications of tetrahydropyrrolo-3,4-azoles and tetrahydropyrrolo-2,3-azoles in medicinal chemistry

Abstract

Tetrahydropyrrolo-3,4-azoles and tetrahydropyrrolo-2,3-azoles represent an interesting family of heterocycles that offer potential utility in drug design as either scaffolds or pharmacophoric elements. The tetrahydropyrrolo[3,4- c ]pyrazole ring system is the most explored representative of this class of heterobicycle which is represented in the marketed dipeptidyl peptidase-4 inhibitor omarigliptin and the Phase 2 clinical candidate danusertib, an Aurora kinase inhibitor. In this chapter, we provide an overview of the synthesis of tetrahydropyrrolo-3,4-azoles and summarize their applications in drug design and discovery. In contrast, the tetrahydropyrrolo-2,3-azole series has been only sparsely explored with no significant systematic study or defined application in drug design.