Highly active ozonides selected against drug resistant malaria
Mem. Inst. Oswaldo Cruz
;
111(7): 450-453, tab
Article
in English
| LILACS
| ID: lil-787558
ABSTRACT
Ever increasing multi-drug resistance by Plasmodium falciparum is creating new challenges in malaria chemotherapy. In the absence of licensed vaccines, treatment and prevention of malaria is heavily dependent on drugs. Potency, range of activity, safety, low cost and ease of administration are crucial issues in the design and formulation of antimalarials. We have tested three synthetic ozonides NAC89, LC50 and LCD67 in vitro and in vivo against multidrug resistant Plasmodium. In vitro, LC50 was at least 10 times more efficient inhibiting P. falciparum multidrug resistant Dd2 strain than chloroquine and mefloquine and as efficient as artemisinin (ART), artesunate and dihydroartemisinin. All three ozonides showed high efficacy in clearing parasitaemia in mice, caused by multi-drug resistant Plasmodium chabaudi strains, by subcutaneous administration, demonstrating high efficacy in vivo against ART and artesunate resistant parasites.
Full text:
Available
Index:
LILACS (Americas)
Main subject:
Plasmodium falciparum
/
Malaria, Falciparum
/
Antimalarials
Limits:
Animals
/
Female
/
Humans
Language:
English
Journal:
Mem. Inst. Oswaldo Cruz
Journal subject:
Tropical Medicine
/
Parasitology
Year:
2016
Type:
Article
/
Project document
Affiliation country:
Portugal
Institution/Affiliation country:
Universidade Nova de Lisboa/PT
Similar
MEDLINE
...
LILACS
LIS