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@article{2243545, author = {Kos, Jiří and Degotte, Gilles and Pindjakova, Dominika and Strhársky, Tomáš and Jankech, Timotej and Goněc, Tomáš and Francotte, Pierre and Frederich, Michel and Jampilek, Josef}, article_location = {Basel}, article_number = {22}, doi = {http://dx.doi.org/10.3390/molecules27227799}, keywords = {cinnamanilides; antiplasmodial activity; Plasmodium; structure-activity relationships}, language = {eng}, issn = {1420-3049}, journal = {Molecules}, title = {Insights into Antimalarial Activity of N-Phenyl-Substituted Cinnamanilides}, url = {https://www.mdpi.com/1420-3049/27/22/7799}, volume = {27}, year = {2022} }
TY - JOUR ID - 2243545 AU - Kos, Jiří - Degotte, Gilles - Pindjakova, Dominika - Strhársky, Tomáš - Jankech, Timotej - Goněc, Tomáš - Francotte, Pierre - Frederich, Michel - Jampilek, Josef PY - 2022 TI - Insights into Antimalarial Activity of N-Phenyl-Substituted Cinnamanilides JF - Molecules VL - 27 IS - 22 SP - 1-10 EP - 1-10 PB - MDPI SN - 14203049 KW - cinnamanilides KW - antiplasmodial activity KW - Plasmodium KW - structure-activity relationships UR - https://www.mdpi.com/1420-3049/27/22/7799 N2 - 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. ER -
KOS, Jiří, Gilles DEGOTTE, Dominika PINDJAKOVA, Tomáš STRHÁRSKY, Timotej JANKECH, Tomáš GONĚC, Pierre FRANCOTTE, Michel FREDERICH a Josef JAMPILEK. Insights into Antimalarial Activity of N-Phenyl-Substituted Cinnamanilides. \textit{Molecules}. Basel: MDPI, 2022, roč.~27, č.~22, s.~1-10. ISSN~1420-3049. Dostupné z: https://dx.doi.org/10.3390/molecules27227799.
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