Table 2. Assay Results for Nitroalkylpyrimidines as Inhibitors of PTR1 and Anti-trypanosomal Activity Against T. b. brucei in Culture and Human HEK Cells.

cpd. no.	R	X	TbPTR1 (Kiapp μM)	T. b. brucei (IC50 μM)	HEK (IC50 μM)
26a	OH	4-Me–C6H4	>100	2.038	73.36
26b	OH	4-F–C6H4	>100	1.857	149.5
26c	OH	H	>100	1.016	134.2
26d	OH	Ph(CH2)2	>100	N/A	NT
28a	NH2	4-Me–C6H4	Insol	0.47	32.45
28b	NH2	4-F–C6H4	∼50	0.16	39.11
28c	NH2	H	Insol	0.13	34.98
28d	NH2	Ph(CH2)2	>100	8.82	NT
30a	Me2CHCH2O–	4-F–C6H4–	>100	13.9 (HMI-9), 10.6 (CMM)	NT
30b	N-cyclohexyl amino	4-F–C6H4–	>100	0.54 (HMI-9), 0.80 (CMM)	32.62
30c	i-PrO	4-F–C6H4–	Insol	15.9 (HMI-9), 8.48 (CMM)	NT