Development of tetrahydroisoquinoline analogues: Towards a treatment for Human African Trypanosomiasis

Abstract

This research describes the exploration of a new scaffold with the potential to be developed in to a new drug for the treatment of Human African Trypanosomiasis (HAT), a neglected disease endemic in sub-Saharan Africa. Derivatives of an isoquinoline scaffold were synthesised and evaluated for their in vitro activity against T.b.rhodesiense, the causative agent of HAT. Five derivatives were identified with inhibition of T.b.rhodesiense in the sub-micromolar range with good selectivity over mammalian cells.