(+)-Usnic acid is a weak antimalarial agent, however, in conjugation with known antimalarial scaffolds and drugs, such as dihydroartemisinin, potent activity against the blood-stage parasite can be seen both in vitro and in vivo. The compound shown exhibits and IC50 of 1.4nM against Plasmodium falciparum in vitro and proved nearly as efficacious as artesunate in a mouse model of infection.
Synthesis of a potent antimalarial agent through natural products conjugation / M. Bruno, B. Trucchi, D. Monti, S. Romeo, M. Kaiser, L. Verotta. - In: CHEMMEDCHEM. - ISSN 1860-7179. - 8:2(2013 Feb), pp. 221-225. [10.1002/cmdc.201200503]
Synthesis of a potent antimalarial agent through natural products conjugation
M. Bruno
;B. TrucchiSecondo
;S. Romeo;L. VerottaUltimo
2013
Abstract
(+)-Usnic acid is a weak antimalarial agent, however, in conjugation with known antimalarial scaffolds and drugs, such as dihydroartemisinin, potent activity against the blood-stage parasite can be seen both in vitro and in vivo. The compound shown exhibits and IC50 of 1.4nM against Plasmodium falciparum in vitro and proved nearly as efficacious as artesunate in a mouse model of infection.
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