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Simultaneous Administration of 2-aminoethyl Diphenylborinate and Chloroquine Reverses Chloroquine Resistance in Malaria Parasites

Ehab Mossaad, Wakako Furuyama, Masahiro Enomoto, Satoru Kawai, Katsuhiko Mikoshiba, Shin-ichiro Kawazu

Antimicrob Agents Chemother. 2015 May;59(5):2890-2.

PMID: 25691631

Abstract:

A nearly complete reversal of chloroquine (CQ) resistance in the CQ-resistant Plasmodium falciparum K-1 strain, with a significant decrease in the mean ± standard deviation (SD) 50% inhibitory concentration (IC50) from 1,050 ± 95 nM to 14 ± 2 nM, was achieved in vitro by the simultaneous administration of 2-aminoethyl diphenylborinate (2-APB). The CQ resistance-reversing activity of 2-APB, which showed the same efficacy as verapamil, was also observed in an in vivo mouse infection model with the CQ-resistant Plasmodium chabaudi AS(30CQ) strain.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP524958 2-Aminoethyl diphenylborinate 2-Aminoethyl diphenylborinate 524-95-8 Price
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