Novel and potent anti-malarial agents.
Readily accessible, novel, and potent anti-malarial compounds have been developed. Optimization of the initial lead structure resulted in derivatives with IC50 values from 7 to 35 nM against chloroquine-sensitive and 70-350 nM against chloroquine-resistant strains of Plasmodium falciparum.
Brinner
Kristin M
KM
Center for New Directions in Organic Synthesis, Chemistry Department, University of California, Berkeley, CA 94720, USA.
Mi Kim
Jin
J
Habashita
Hiromu
H
Gluzman
Ilya Y
IY
Goldberg
Daniel E
DE
Ellman
Jonathan A
JA
D000478:Alkylation; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology*; D002478:Cells, Cultured; D002738:Chloroquine / Q000494:pharmacology; D004351:Drug Resistance; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D010963:Plasmodium falciparum / Q000187:drug effects*; D013329:Structure-Activity Relationship
D000962:Antimalarials; D007202:Indicators and Reagents; D002738:Chloroquine