- Structure-activity relationship in cinnamamides. 3. Synthesis and anticonvulsant activity evaluation of some derivatives of (E)- and (Z)-m-(trifluoromethyl)cinnamamide
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The (E)- and (Z)-m-(trifluoromethyl)-α,β-dimethylcinnamamides and some of their N-alkyl derivatives were prepared and pharmacologically tested as anticonvulsant agents in order to verify if a ring substituent, like the m-CF3 group, different from a halogen but possessing the same electronic effect could lead to equally active compounds. Some (E)-m-(trifluoromethyl)-α-methyl- and -non-methyl-substituted-cinnamamides were also prepared and tested. In the α,β-dimethyl series, the results show that the m-CF3 group leads to products more active than the ones unsubstituted on the phenyl ring but still less active than the p-halogen-substituted compounds previously studied. In the α-methyl and non-methyl-substituted series, the trend shows the m-CF3 group being able to produce less toxic and, in some cases, more active products than the previously studied amides.
- Balsamo,Crotti,Lapucci,Macchia,Macchia,Cuttica,Passerini
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p. 525 - 532
(2007/10/02)
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- 3-Fluoro-N-cyclopropylcinnamide
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Cinnamamides of formula (I), STR1 wherein X is fluoro, chloro, bromo, iodo or trifluoromethyl and R is cycloalkyl or cycloalkyl alkyl, have anticonvulsant properties. The compound trans-3-fluoro-(N-cyclopropyl)cinnamamide is also useful as a muscle relaxa
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