Table 2.

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

		Potency (μM) Ave. ± S.E.M. (n= 4)
Compound	R	PfG6PD Primary Assay	PfG6PD NADPH Kinetic
5a	2-F	1.73 ± 0.08	1.37
5b	H	8.23 ± 2.11	19.7
6b	2-Cl	2.56 ± 0.19	3.3
5c	2-Me	5.93 ± 1.59	5.01
5d	2-OMe	9.79 ± 1.13	11.3
5e	3-F	2.35 ± 0.29	4.13
5f	4-F	1.41 ± 0.14	2.06
7b	4-Me	4.42 ± 0.71	11.6
5g	2,3-difluoro	5.72 ± 1.28	3.89
5h	2,6-difluoro	1.65 ± 0.08	2.61
5i	1-napthyl	4.28 ± 0.87	4.2
5j	2-napthyl	2.39 ± 0.28	2.88

^aall compounds represented in this table exhibited an IC₅₀ > 80 μM against human G6PD

^bscreen hit