Reversal agent and linker variants of reversed chloroquines: activities against Plasmodium falciparum.
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.
Andrews
Simeon
S
Department of Chemistry, Portland State University, P.O. Box 751, Portland, Oregon 97207-0751, USA.
Burgess
Steven J
SJ
Skaalrud
Deborah
D
Kelly
Jane Xu
JX
Peyton
David H
DH
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
D000962:Antimalarials; D010879:Piperazines; D002738:Chloroquine