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Updated: Jun 9, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Bis-alkylamine quindolone derivatives as new antimalarial leads
João Lavrado1, Kaamil Gani, Pedro A Nobre
1iMed.UL, Faculdade de Farmácia, Universidade de Lisboa, Av Prof Gama Pinto 1649-003 Lisboa, Portugal.
Abstract:
Quindolone derivatives, designed to target the malaria parasite digestive vacuole and heme detoxification pathway, have been synthesized by reaction with 2-chloro-N,N-diethylethanamine. This reaction gave N,O-, N,N- and O-alkylated products containing one or two basic side-chains. The compounds were evaluated for antiplasmodial activity against the chloroquine-resistant Plasmodium falciparum W2 strain and for cytotoxicity in HepG2 A16 hepatic cells. By incorporating alkylamine side chains and chlorine atoms in the quindolone nucleus we transformed the inactive tetracyclic parent quindolones into moderate or highly active and selective antimalarial compounds. The most active and selective compound, 5c, showed an IC(50)=51 nM for P. falciparum and a selectivity ratio of 98.
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