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. Author manuscript; available in PMC: 2019 Apr 13.
Published in final edited form as: ACS Infect Dis. 2017 Nov 7;4(4):549–559. doi: 10.1021/acsinfecdis.7b00159

Table 1.

Pf IspD Inhibition Potency of MMV008138 Stereoisomers and FOS

graphic file with name nihms918690u2.jpg
compound configuration P. falciparum growth inhibition IC50 (nM)a % recovery (200 μM IPP)c PfIspD IC50 (nM)d % E. coli growth inhibition (18 h)e
1a (1R,3S) 250 ± 70b 100 @ 2.5 μMb 44 ± 15 NI @ 500 μMb
5a (1S,3S) >10 000b NDb NI @ 1 μM NI @ 125 μM
ent-1a (1S,3R) >10 000b NDb NI @ 1 μM NI @ 250 μM
ent-5a (1R,3R) 3000 ± 200b 60 ± 5 @ 10 μMb 27 ± 5% inh. @ 1 μM 18 ± 6 @ 250 μM
FOS NA 880 ± 70b 100b 4 ± 2% inh. @ 10 μM 11.99 ± 0.02 μM (MIC)
a

MRA-150, chloroquine-resistant (intermediate), pyrimethamine-resistant, mefloquine-resistant.

b

Data reported previously.13

c

Drug at indicated concentration.

d

Recombinant P. falciparum IspD IC50 values measured at 60 nM Pf IspD.

e

Percent growth inhibition at the indicated concentration or the minimum inhibitory concentration (MIC). Values represent averages of at least two independent assays ± SEM. NA signifies “not applicable”. ND signifies “not determined”. NI signifies “no inhibition”.