Table 2. Compound 50–69 with amide linker at R³.

ID	R3 (para)	R3 (meta)	MW	clog Da	LEb	LLEc	Pf3D7 IC50 (μM)	HepG2 IC50 (μM)	SI
50		H	427.5	3.50	0.29	3.38	0.14 ± 0.05	6.4 ± 2.4	46.5
51	H		427.5	3.52	0.29	3.15	0.22 ± 0.09	10.6 ± 6.0	47.5
52		H	456.6	2.71	0.27	4.09	0.16 ± 0.04	11.5 ± 1.5	70.9
53	H		456.6	2.71	0.25	3.52	0.60 ± 0.04	18.1 ± 2.6	30.4
54		H	510.7	1.24	0.24	5.44	0.22 ± 0.07	13.6 ± 2.6	62.6
55	H		510.7	1.24	0.24	5.54	0.17 ± 0.001	13.9 ± 1.8	82.6
56		H	415.5	2.25	0.28	4.01	0.56 ± 0.1	8.9 ± 0.9	15.9
57	H		415.5	2.25	0.27	3.89	0.73 ± 0.2	21.7 ± 2.5	29.6
58		H	427.5	3.09	0.25	2.72	1.6 ± 0.09	18.8 ± 0.3	12.1
59	H		427.5	3.10	0.25	2.84	1.2 ± 0.2	20.4 ± 0.7	17.6
60		H	413.5	2.50	0.27	3.69	0.65 ± 0.06	48.2 ± 13.2	73.9
61	H		413.5	2.50	0.27	3.62	0.77 ± 0.2	23.7 ± 5.4	30.9
62		H	414.5	3.38	0.23	1.73	8.2 ± 3.4	28.7 ± 4.2	3.5
63	H		414.5	3.38	0.24	2.15	3.0 ± 0.9	54.4 ± 23.2	17.9
64		H	481.6	1.98	0.25	4.52	0.32 ± 0.03	24.5 ± 7.1	77.7
65	H		481.6	2.01	0.23	4.14	0.71 ± 0.2	23.6 ± 8.3	33.2
66		H	399.5	1.89	0.28	4.32	0.63 ± 0.2	23.5 ± 7.5	37.1
67	H		399.5	1.89	0.28	4.28	0.69 ± 0.2	11.7 ± 3.4	17
68		H	467.6	2.00	0.28	5.19	0.060 ± 0.004	8.7 ± 0.3	135.7
69	H		467.6	2.03	0.29	5.26	0.050 ± 0.004	5.2 ± 0.8	101.2

^aChemAxon JChem 24.1.2.

^bLE = (1.37 × Pf pIC₅₀)/(heavy atoms).

^cLLE = (Pf pIC₅₀ − clog D).