From a methanolic extract of the leaves of Andira inermis (Fabaceae), andirol A and B, two compounds with a novel type of a rotenoid-related skeleton and andinermol, a new 2-aryl-3-hydroxymethyl-benzofuran could be isolated. Characterisation and structure elucidation of these compounds was achieved on the basis of their spectral data. In addition, the in vitro activities of the isolated compounds against both the chloroquine-sensitive strain PoW and the chloroquine-resistant clone Dd2 of Plasmodium falciparum have been evaluated.