Synthesis and evaluation of phenylequine for antimalarial activity in vitro and in vivo |
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| Authors: | Margaret A.L. Blackie Vanessa Yardley Kelly Chibale |
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| Affiliation: | 1. Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa;2. Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, UK;3. Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa |
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| Abstract: | Synthesis of the potent antiplasmodial 4-aminoquinoline, phenylequine (PQ), is reported for the first time. PQ and the two analogues show increased efficacy in moving from the chloroquine sensitive D10 to the chloroquine resistant K1 strain in vitro. The in vivo efficacy of PQ, and salts thereof, have been determined in Plasmodium berghei ANKA and Plasmodium yoelii. Phenylequine hydrochloride has shown an ED50 of 0.81 in P. yoelii (cf chloroquine ED50 = 1.31). |
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