Structure-activity relationships in a series of antiplasmodial thieno[2,3-b]pyridines.

ABSTRACT:

Background

Malaria is one of the most prevalent tropical infectious diseases. Since recently cases of artemisinin resistance were reported, novel anti-malarial drugs are required which differ from artemisinins in structure and biological target. The plasmodial glycogen synthase kinase-3 (PfGSK-3) was suggested as a new anti-malarial drug target. 4-Phenylthieno[2,3-b]pyridines were previously identified as selective PfGSK-3 inhibitors with antiplasmodial activity. The present study aims at identifying a molecular position on this scaffold for the attachment of side chains in order to improve solubility and antiplasmodial activity. Furthermore, the role of axial chirality in the compound class for antiplasmodial activity and PfGSK-3 inhibition was investigated.

Methods

4-Pheny

SUBMITTER: Masch A 

PROVIDER: S-EPMC6429710 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature