Statine-based inhibitors of Plasmepsin II (PLMII) coupled with Primaquine have been designed using the ‘double-drug' approach. The IC50 values for PLMII inhibition ranged from 0.59 to 400 nM and the best IC50 value for inhibition of Plasmodium falciparum growth in vitro was 0.4 μM, which represent a remarkable improvement compared to other statine-based PLMII inhibitors.
Plasmepsin II inhibition and antiplasmodial activity of Primaquine-Statine 'double-drugs' / S. Romeo, M. Dell'Agli, S. Parapini, L. Rizzi, G. Galli, M. Mondani, A.C. Sparatore, D. Taramelli, E.A. Bosisio. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 14:11(2004), pp. 2931-2934.
Plasmepsin II inhibition and antiplasmodial activity of Primaquine-Statine 'double-drugs'
S. RomeoPrimo
;M. Dell'AgliSecondo
;S. Parapini;L. Rizzi;G. Galli;M. Mondani;A.C. Sparatore;D. TaramelliPenultimo
;E.A. BosisioUltimo
2004
Abstract
Statine-based inhibitors of Plasmepsin II (PLMII) coupled with Primaquine have been designed using the ‘double-drug' approach. The IC50 values for PLMII inhibition ranged from 0.59 to 400 nM and the best IC50 value for inhibition of Plasmodium falciparum growth in vitro was 0.4 μM, which represent a remarkable improvement compared to other statine-based PLMII inhibitors.
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