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Synthesis of a Potent Antimalarial Agent through Natural Products Conjugation
Author(s) -
Bruno Michela,
Trucchi Beatrice,
Monti Diego,
Romeo Sergio,
Kaiser Marcel,
Verotta Luisella
Publication year - 2013
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201200503
Subject(s) - antimalarial agent , combinatorial chemistry , chemistry , malaria , natural (archaeology) , stereochemistry , artemisinin , pharmacology , plasmodium falciparum , biology , immunology , paleontology
Au naturel! (+)‐Usnic acid (green) is a weak antimalarial agent, however, in conjugation with known antimalarial scaffolds and drugs, such as dihydroartemisinin (blue), potent activity against the blood‐stage parasite can be seen both in vitro and in vivo. The compound shown exhibits an IC 50 value of 1.4 n M against Plasmodium falciparum in vitro and proved nearly as efficacious as artesunate in a mouse model of infection.