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. Author manuscript; available in PMC: 2019 Oct 11.
Published in final edited form as: J Med Chem. 2018 Sep 24;61(19):8847–8858. doi: 10.1021/acs.jmedchem.8b01026

Table 2.

Growth Inhibition of the Analogues against P. falciparuma

graphic file with name nihms-993383-f0003.jpg

compd R1 R2 R3 Pf DXR IC50 [μM]
1a 1.087 ± 0.064
1b 0.511 ± 0.0535
2 Na/H H CH3 0.202 ± 0.01535
3 POM H CH3 0.018 ± 0.00235
12a Na/H H H 0.019 ± 0.002
12b Na/H H CF3 113.3 ± 22.4
12c NH4 H OCH3 28.6 ± 5.0
16d Na/H CH(CH3)Ph CH3 1.2 ± 0.1
16e Na/H CH2(4-iprPh) CH3 1.1 ± 0.0
16f Na/H CH2(2-naphthyl) CH3 26.1 ± 1.1
16g Na/H CH2(4-biphenyl) CH3 2.3 ± 0.4
18a POM H H 0.013 ± 0.002
18b POM H CF3 14.3 ± 2.5
18c POM H OCH3 23.7 ± 6.6
19e POM CH2(4-iprPh) CH3 55.2 ± 1.9
19f POM CH2(2-naphthyl) CH3 50.5 ± 1.1
19g POM CH2(4-biphenyl) CH3 44.1 ± 1.1
a

Pf = P. falciparum; IC50 = concentration giving 50% inhibition of Pf growth