Plasmodium Falciparum: Role of Absolute Stereochemistry in the Antimalarial Activity of Synthetic Amino Alcohol Antimalarial Agents
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 anti agents containing a piperidine ring. The enantiomers of amino-alcohol antimalarial agents in which the amine is part of an acrylic group, such as in halofantrine, displayed little, if any, differential antimalarial activity. Thus, the effect of absolute stereochemistry of the amino alcohol antimalarial agents on antimalarial activity appears to depend upon both the flexibility of the amine portion of the molecule and the structure of the aromatic portion of the molecule.
Document Details
- Document Type
- Technical Report
- Publication Date
- Jan 01, 1993
- Accession Number
- ADA269099
Entities
People
- J. M. Karle
- L. Gerena
- R. Olmeda
- W. K. Milhous
Organizations
- Walter Reed Army Institute of Research