Synthesis of tetrahydro-β-carboline analogs with N11 modifications and study of their antimalarial activities

Abstract

Tetrahydro-β-carbolines are medicinal important class of compounds have their place in indole family. N-benzylation variations at indole of Tetrahydro-β-Carboline’s needs to explored of its pharmacological activities. Seventeen N-11-benzylic- β-carboline derivatives were synthesized from 2-(5-methoxy-1H-indol-3-yl)-2-oxoacetaldehyde and 2-(5-methoxy-1H-indol-3-yl)ethan-1-amine (N-alkylated) via Pictet–Spengler reaction and Keto reduction using LiCl/NaBH₄, including eleven N-substituted and six Keto reduced β-carboline derivatives. Antimalarial activities of these analogs were studied on 3D7 and C580Y parasite strains.