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. Author manuscript; available in PMC: 2013 Aug 23.
Published in final edited form as: J Med Chem. 2012 Aug 6;55(16):7262–7272. doi: 10.1021/jm300833h

Table 4.

SAR of benzothiazinones inhibiting Plasmodium falciparum glucose-6-phosphate dehydrogenase

graphic file with name nihms397376u2.jpg Potency (μM) Ave. ± S.E.M.
Entry R1 R2 Yield % PfG6PD Primary Assay PfG6PD NADPH Kinetic
5a
racemic 		graphic file with name nihms397376t9.jpg 2-F 19 1.7 ± 0.1 1.4
11
R-enantiomer
ML276 		graphic file with name nihms397376t10.jpg 2-F 32 0.9 ± 0.0 1.9
12
S-enantiomer 		graphic file with name nihms397376t11.jpg 2-F 28 6.6 ± 0.2 4.7
13 graphic file with name nihms397376t12.jpg 2-F 48 3.1 ± 0.4 4.0
14 graphic file with name nihms397376t13.jpg 2-F 61 >80.0 24.4
15 graphic file with name nihms397376t14.jpg 2-F 79 5.9 ± 0.6 5.0