Aminoquinolines That Circumvent Resistance in Plasmodium falciparum in Vitro
| Autor: | Frances M. Krogstad, Donald J. Krogstad, Frank B. Cogswell, Dibyendu De |
|---|---|
| Rok vydání: | 1996 |
| Předmět: |
Stereochemistry
Plasmodium falciparum Drug Resistance Biology Pharmacology Aminoquinoline Antimalarials Structure-Activity Relationship Chloroquine Virology parasitic diseases medicine Animals Humans Structure–activity relationship Aminoquinolines Mefloquine Biological activity Calcium Channel Blockers biology.organism_classification Infectious Diseases Verapamil Parasitology Isopropyl medicine.drug |
| Zdroj: | The American Journal of Tropical Medicine and Hygiene. 55:579-583 |
| ISSN: | 1476-1645 0002-9637 |
| DOI: | 10.4269/ajtmh.1996.55.579 |
| Popis: | Aminoquinoline (AQ) resistance is one of the most important factors in the worldwide resurgence of malaria due to Plasmodium falciparum. We synthesized a series of AQs to define the structure-activity relationships responsible for AQ action against chloroquine-susceptible and -resistant P. falciparum. The AQs with ethyl, propyl, isopropyl, butyl, pentyl, isopentyl (chloroquine), hexyl, octyl, decyl, or dodecyl side chains were equally active against chloroquine-susceptible P. falciparum (50% inhibitory concentrations [IC50s] = 5–15 nM). The AQs with ethyl, propyl, isopropyl, decyl, or dodecyl side chains were also active against chloroquine-, mefloquine- and multiply-resistant P. falciparum (IC50s = 5–20 nM). Verapamil, which enhances the activity of chloroquine against chloroquine-resistant parasites, had no effect on the activity of AQs that were active against resistant parasites. These results indicate that AQs with 2–12 carbon side chains are as active as chloroquine against chloroquine-susceptible P. falciparum, and that AQs with side chains shorter or longer than chloroquine are often active against chloroquine-, mefloquine-, and multiply-resistant P. falciparum. |
| Databáze: | OpenAIRE |
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