title: Reversal agent and linker variants of reversed chloroquines: activities against Plasmodium falciparum.
abstract: We have shown that "reversed chloroquine molecules" constructed from chloroquine-like and resistance "reversal-agent"-like cores can be powerful drugs against malaria ( J. Med. Chem. 2006 , 49 , 5623 - 5625 ). Several reversed chloroquines are now presented that probe parameters governing the activities against chloroquine-resistant and chloroquine-sensitive malaria strains. The design is tolerant to linker and reversal agent changes, but a piperazinyl group adjacent to the quinoline, at least for the group of compounds studied here, may be detrimental.
authors.affiliation: Department of Chemistry, Portland State University, P.O. Box 751, Portland, Oregon 97207-0751, USA.
authors.forename: Simeon
authors.initials: S
authors.lastname: Andrews
authors.forename: Steven J
authors.initials: SJ
authors.lastname: Burgess
authors.forename: Deborah
authors.initials: D
authors.lastname: Skaalrud
authors.forename: Jane Xu
authors.initials: JX
authors.lastname: Kelly
authors.forename: David H
authors.initials: DH
authors.lastname: Peyton
mesh_terms: D000962:Antimalarials / Q000737:chemistry*; D002738:Chloroquine / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D015195:Drug Design; D004351:Drug Resistance; D010879:Piperazines; D010963:Plasmodium falciparum / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D010879:Piperazines; D002738:Chloroquine