Impact of Nanoparticles on Protozoa

Plachá, Daniela; Jampílek, Josef

doi:10.1002/9781119769897.ch4

Cited by 2 publications

(2 citation statements)

References 172 publications

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“…A major cause of concern is the emergence of resistant and multidrug-resistant strains in Africa, including isolates resistant to chloroquine and artemisinin [6,7]. Another undesirable fact is that, due to climate change, the parasite and its vectors could spread to areas where they were eradicated or not present before [8,9]. In 2020, nearly half of the world's population was at risk of malaria [5].…”

Section: Introductionmentioning

confidence: 99%

Insights into Antimalarial Activity of N-Phenyl-Substituted Cinnamanilides

et al. 2022

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Due to the urgent need of innovation in the antimalarial therapeutic arsenal, a series of thirty-seven ring-substituted N-arylcinnamanilides prepared by microwave-assisted synthesis were subjected to primary screening against the chloroquine-sensitive strain of P. falciparum 3D7/MRA-102. The lipophilicity of all compounds was experimentally determined as the logarithm of the capacity factor k, and these data were subsequently used in the discussion of structure-activity relationships. Among the screened compounds, fourteen derivatives exhibited IC50 from 0.58 to 31 µM, whereas (2E)-N-(4-bromo-2-chlorophenyl)-3-phenylprop-2-enamide (24) was the most effective agent (IC50 = 0.58 µM). In addition, (2E)-N-[2,6-dibromo-4-(trifluoromethyl)- phenyl]-3-phenylprop-2-enamide (36), (2E)-N-[4-nitro-3-(trifluoromethyl)phenyl]-3-phenylprop- 2-enamide (18), (2E)-N-(2-bromo-5-fluorophenyl)-3-phenylprop-2-enamide (23), and (2E)-3-phenyl-N-(3,4,5-trichlorophenyl)prop-2-enamide (33) demonstrated efficacy in the IC50 range from 2.0 to 4.3 µM, comparable to the clinically used standard chloroquine. The results of a cell viability screening performed using THP1-Blue™ NF-κB cells showed that none of these highly active compounds displayed any significant cytotoxic effect up to 20 μM, which makes them promising Plasmodium selective substances for further investigations.

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