Related Experiment Video
Updated: Apr 5, 2026

Optimized Griess Reaction for UV-Vis and Naked-eye Determination of Anti-malarial Primaquine
Published on: October 11, 2019
Exploring the 3-piperidin-4-yl-1H-indole scaffold as a novel antimalarial chemotype
Sofia A Santos1, Amanda K Lukens2, Lis Coelho3
1Research Institute for Medicines (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, Av. Professor Gama Pinto, 1640-003 Lisbon, Portugal; Center for Systems Biology, Massachusetts General Hospital, Boston, MA 02114, USA.
Abstract:
A series of 3-piperidin-4-yl-1H-indoles with building block diversity was synthesized based on a hit derived from an HTS whole-cell screen against Plasmodium falciparum. Thirty-eight compounds were obtained following a three-step synthetic approach and evaluated for anti-parasitic activity. The SAR shows that 3-piperidin-4-yl-1H-indole is intolerant to most N-piperidinyl modifications. Nevertheless, we were able to identify a new compound (10d) with lead-like properties (MW = 305; cLogP = 2.42), showing antimalarial activity against drug-resistant and sensitive strains (EC50 values ∼ 3 μM), selectivity for malaria parasite and no cross-resistance with chloroquine, thus representing a potential new chemotype for further optimization towards novel and affordable antimalarial drugs.
More Related Videos
Related Concept Videos
Basicity of Heterocyclic Aromatic Amines
Antifungal Agents
Nomenclature of Aryl and Heterocyclic Amines
Anthelminthic Agents

