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Acaricidal activity of tonka bean extracts. Synthesis and structure-activity relationships of bioactive derivatives
Christophe Gleye1, Guy Lewin, Alain Laurens
1Laboratoire de Pharmacognosie, UMR 8076 CNRS (BioCIS), Faculté de Pharmacie, Université Paris XI, 92296 Châtenay-Malabry Cedex, France.
Abstract:
The acaricidal effects of tonka bean, Dipterix odorata, extracts were investigated on Dermatophagoides pteronyssinus, the European house dust mite, and compared with benzyl benzoate as a standard acaricidal compound. A cyclohexane extract was the most effective, with an EC(50) = 0.075 g/m(2) after a 24 h period, as compared with benzyl benzoate (0.025 g/m(2)). Bioassay-guided fractionation of this extract led to the isolation of coumarin (1). Pharmacomodulation of this compound led us to test 20 analogues (2-21), which were either synthesized or purchased.
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