Table 1. Inhibition by O-3 derivatives of d-glucose on hexose transport mediated by PfHT in oocytes and on cultured P. falciparum.
C3 analogue | KI for D-glucose uptake | KI for D-fructose uptake | IC50 (P. falciparum growth) |
---|---|---|---|
3-O-ethyl-D-glucose | 1.62 ± 0.72 | 2.67 ± 0.66 | 3.70 ± 1.041 |
3-O-benzyl-D-glucose | 2.19 ± 0.85 | 1.49 ± 0.93 | 5.23 ± 1.063 |
3-O-hydroxyethyl-D-glucose | 14.8 ± 1.4 | > 10 | > 10 |
3-O-((undec-10-en)-1-yl)-D-glucose (compound 3361) | 0.053 ± 0.019 | 0.027 ± 0.003 | 0.0157 ± 0.0017 |
Experiments were performed on strain 3D7 with 4 mM D-glucose. Values (mean ± SE of three independent replicates) are expressed in mM.