Abstract
The high cost and protracted time line of new drug discovery are major roadblocks to creating therapies for neglected diseases. To accelerate drug discovery we created a library of 2,687 existing drugs and screened for inhibitors of the human malaria parasite Plasmodium falciparum. The antihistamine astemizole and its principal human metabolite are promising new inhibitors of chloroquine-sensitive and multidrug-resistant parasites, and they show efficacy in two mouse models of malaria.
Publication types
-
Research Support, N.I.H., Extramural
-
Research Support, Non-U.S. Gov't
-
Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
-
Animals
-
Antimalarials / adverse effects
-
Antimalarials / metabolism
-
Antimalarials / pharmacology*
-
Astemizole / adverse effects
-
Astemizole / analogs & derivatives*
-
Astemizole / metabolism
-
Astemizole / pharmacology*
-
Chloroquine / pharmacology
-
Disease Models, Animal
-
Dose-Response Relationship, Drug
-
Drug Evaluation, Preclinical
-
Drug Resistance
-
Drug Resistance, Multiple
-
Humans
-
Mice
-
Plasmodium falciparum / drug effects*
-
Plasmodium yoelii / drug effects
Substances
-
Antimalarials
-
Astemizole
-
Chloroquine
-
desmethylastemizole
Associated data
-
PubChem-Substance/11538010
-
PubChem-Substance/11538011
-
PubChem-Substance/11538012
-
PubChem-Substance/11538013
-
PubChem-Substance/11538014
-
PubChem-Substance/11538015