(+)-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. Trucchi
Secondo
;
S. Romeo;L. Verotta
Ultimo
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.
antiprotozoal agents; drug discovery; Mannich bases; medicinal chemistry; usnic acids
Settore CHIM/06 - Chimica Organica
Settore CHIM/08 - Chimica Farmaceutica
feb-2013
gen-2013
Article (author)
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/215678
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