Plasmodium falciparum: role of absolute stereochemistry in the antimalarial activity of synthetic amino alcohol antimalarial agents
JM Karle, R Olmeda, L Gerena, WK Milhous - Experimental parasitology, 1993 - Elsevier
Abstract The (+)-isomers of mefloquine and its threo analog are 1.69 to 1.95 times more
active than the (−)-isomers against chloroquine-sensitive and chloroquine-resistant
Plasmodium falciparum in vitro. This large a differential between the activity of (+)-and (−)-
isomers was not observed for other synthetic amino alcohol antimalarial agents containing a
piperidine ring. The enantiomers of amino alcohol antimalarial agents in which the amine is
part of an acyclic group, such as in halofantrine, displayed little, if any, differential …
active than the (−)-isomers against chloroquine-sensitive and chloroquine-resistant
Plasmodium falciparum in vitro. This large a differential between the activity of (+)-and (−)-
isomers was not observed for other synthetic amino alcohol antimalarial agents containing a
piperidine ring. The enantiomers of amino alcohol antimalarial agents in which the amine is
part of an acyclic group, such as in halofantrine, displayed little, if any, differential …