[1,2,4]triazolo[4,3-a]quinazolin-5-one deriva tives as antimalarial agents

S. Yu. Danylchenko, S. S. Kovalenko, O. G. Drushlyak, S. M. Kovalenko, L. Maes


Five novel [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one derivatives containing an amide group connected to 1 position of triazoloquinazoline moiety via sulfur-carbon or carbon chain were synthesized. The structure was confirmed by elemental analysis and 1H NMR spectroscopy. Their in vitro antiprotozoal activity was evaluated against Leishmania infantum, Plasmodium falciparum, Trypanosoma brucei and Trypanosoma cruzi. 4-Benzyl-1-{4-[4-(4-methoxyphenyl)piperazin-1-yl]-4-oxobutyl}[1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one 7e with an amide group connected via carbon chain showed noticeable antimalarial activity (IC50 0.2 µM). The lead structure 7 e may be promising for further investigations as novel antimalarial agents.


2-hydrazinoquinazolin-4(3H)-ones; [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-ones; in vitro; antiprotozoal; antimalaria activity

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