title: Modifications of the alpha,beta-double bond in chalcones only marginally affect the antiprotozoal activities.
abstract: Methods for selective alkylation of chalcones in the alpha- or beta-position and for selective reduction of the alpha,beta-double bond have been developed. The antiparasitic potencies of the alpha,beta-double bond modified chalcones only differ marginally from the potencies of the parent chalcones indicating that the propenone residue only functions as a spacer between the two benzene rings, which are the true pharmacophore.
authors.affiliation: Department of Medicinal Chemistry, Royal Danish School of Pharmacy, and State Serum Institute, Copenhagen.
authors.forename: S F
authors.initials: SF
authors.lastname: Nielsen
authors.forename: A
authors.initials: A
authors.lastname: Kharazmi
authors.forename: S B
authors.initials: SB
authors.lastname: Christensen
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000737:chemistry* / Q000494:pharmacology; D002599:Chalcone / Q000031:analogs & derivatives* / Q000737:chemistry* / Q000494:pharmacology; D004912:Erythrocytes / Q000187:drug effects / Q000469:parasitology; D018320:Leishmania major / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000962:Antimalarials; D014344:Trypanocidal Agents; D002599:Chalcone