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Synthesis of Triazole-linked 2-Trichloromethylquinazolines and Exploration of Their Efficacy Against P. falciparum


AR Hamann
C de Kock
PJ Smith
WAL van Otterlo
MAL Blackie

Abstract

Using 2-trichloromethylquinazoline as scaffold, seven novel triazole-linked compounds have been synthesized using CuAAC chemistry. The in vitro biological activity of four of the compounds on the Plasmodium falciparum chloroquine-sensitive strain NF54 was then determined. The compounds which were tested showed moderate activity with 1.45 μM as the lowest inhibitory concentration.

KEYWORDS Malaria, 2-trichloromethylquinazoline, copper click chemistry, 1,2,3-triazole.


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eISSN: 1996-840X
print ISSN: 0379-4350