Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities.
A simple two-step synthesis method was used to make 51 B-ring-substituted 4-hydroxyquinolines allowing analysis of the effect of ring substitutions on inhibition of growth of chloroquine sensitive and resistant strains of Plasmodium falciparum, the dominant cause of malaria morbidity. Substituted quinoline rings other than the 7-chloroquinoline ring found in chloroquine were found to have significant activity against the drug-resistant strain of P. falciparum W2.
Madrid
Peter B
PB
Department of Pharmaceutical Chemistry, University of California, San Francisco, CA 94143-2280, USA.
Sherrill
John
J
Liou
Ally P
AP
Weisman
Jennifer L
JL
Derisi
Joseph L
JL
Guy
R Kiplin
RK
D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D002738:Chloroquine / Q000494:pharmacology; D004351:Drug Resistance; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship
D000634:Aminoquinolines; D000962:Antimalarials; D002738:Chloroquine; C001920:4-aminoquinoline