title: Conformationally restricted anti-plasmodial chalcones.
abstract: Chalcones can exist as Z- or E-isomers and it is generally anticipated that both isomers are equipotent. In order to determine the active isomer of anti-plasmodial chalcones a series of analogues locked in the Z- or the E-form were prepared and evaluated for their anti-plasmodial activity. It was shown that the Z-locked analogue was nearly inactive, whereas the E-locked analogues were equipotent to the parent chalcones, indicating that the E-isomer is the active conformation.
authors.affiliation: Lica Pharmaceuticals A/S, Symbion Science Park, Fruebjergvej 3, DK-2100 Copenhagen, Denmark.
authors.forename: Mogens
authors.initials: M
authors.lastname: Larsen
authors.forename: Hasse
authors.initials: H
authors.lastname: Kromann
authors.forename: Arsalan
authors.initials: A
authors.lastname: Kharazmi
authors.forename: Simon Feldbaek
authors.initials: SF
authors.lastname: Nielsen
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D047188:Chalcones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008968:Molecular Conformation; D010963:Plasmodium falciparum / Q000187:drug effects*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D047188:Chalcones