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

Abstract

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 1 H 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 (IC 50 0.2 µM). The lead structure 7e may be promising for further investigations as novel antimalarial agents.

A Novel Series of [1,2,4]Triazolo[4,3-a]Pyridine Sulfonamides as Potential Antimalarial Agents: In Silico Studies, Synthesis and In Vitro Evaluation

“…As a follow up to our previous study [ 10 ], in collaboration with Laboratory of Microbiology, Parasitology and Hygiene, University of Antwerp, we paid attention to triazolopyridine scaffold bearing sulfonamide group as chemical entity with potential antimalarial activity. Triazolopyridines represents an important class of heteroaromatic compounds with a wide range of pharmaceutical and biological activities including antibacterial, antifungal [ 11 ], anti-inflammatory [ 12 , 13 , 14 ], herbicidal [ 15 ] and pesticidal [ 16 ], anticonvulsant [ 17 ], anxiolytic [ 18 ], and antipsychotic [ 19 ].…”