Indole-2-carboxamides Optimization for Antiplasmodial Activity.

ABSTRACT: Malaria still stands out as one of the most devastating and prevalent diseases globally, where the rise of resistance to different antimalarial drugs in different regions has posed significant obstacles to global treatment and elimination. Consequently, there is a pressing need for the development of new antimalarial agents with novel modes of action. In this study, we report the identification and optimization of new indole-2-carboxamide derivatives where structural modifications have yielded new compounds 6x with enhanced potency (Pf3D7-IC50 ∼ 0.3 μM) and improved metabolic stability (hMics = 3 μL/min/mg), while also minimizing the human ether-a-go-go-related gene (hERG, IC₅₀ > 20 μM) channel activity and cytotoxic effect on hepatic cells (CC₅₀ > 30 μM

SUBMITTER: Kumar M 

PROVIDER: S-EPMC12531871 | biostudies-literature | 2025 Oct

REPOSITORIES: biostudies-literature