A series of seventeen 4-chlorocinnamanilides and seventeen 3,4-dichlorocinnamanilides were characterized for their antiplasmodial activity. In vitro screening on a chloroquine-sensitive strain of 3D7/MRA-102 highlighted that 23 compounds possessed IC < 30 µM. Typically, 3,4-dichlorocinnamanilides showed a broader range of activity compared to 4-chlorocinnamanilides.
View Article and Find Full Text PDFA series of thirty-two anilides of 3-(trifluoromethyl)cinnamic acid (series ) and 4-(trifluoromethyl)cinnamic acid (series ) was prepared by microwave-assisted synthesis. All the compounds were tested against reference strains ATCC 29213 and ATCC 29212 and resistant clinical isolates of methicillin-resistant (MRSA) and vancomycin-resistant (VRE). All the compounds were evaluated in vitro against ATCC 700084 and CAMP 5644.
View Article and Find Full Text PDFDue to the urgent need of innovation in the antimalarial therapeutic arsenal, a series of thirty-seven ring-substituted -arylcinnamanilides prepared by microwave-assisted synthesis were subjected to primary screening against the chloroquine-sensitive strain of 3D7/MRA-102. The lipophilicity of all compounds was experimentally determined as the logarithm of the capacity factor , and these data were subsequently used in the discussion of structure-activity relationships. Among the screened compounds, fourteen derivatives exhibited IC from 0.
View Article and Find Full Text PDFPattern 1-hydroxy-N-(2,4,5-trichlorophenyl)-2-naphthamide and the thirteen original carbamates derived from it were prepared and characterized. All the compounds were tested against Staphylococcus aureus ATCC 29213 as a reference and quality control strain and in addition against three clinical isolates of methicillin-resistant S. aureus (MRSA).
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