Table 2.

Profile of diaryl ureas tested for in vitro activity against cultured P. falciparum strains and in vivo efficacy in a P. berghei mouse model.

Compound	Ar	R	EC50 3D7 (μM)	EC50 Dd2 (μM)	SC Dose (mg/kg)	FSurvival @ 31da,b,c
14	1-naphthyl	CF3	1.2	0.81	256	NES
15	2-naphthyl	CF3	0.61	0.41	256	NES
16	4-ClPh	Cl	2.0	5.0	256	NES
17	3,4-Cl2Ph	Cl	1.9	2.5	256	NES
18	3-CF3-4-ClPh	CF3	0.037	0.055	256	4/7
18					128	EXT
19	3-CF3-4-FPh	CF3	0.13	0.15	256	1/7
19					128	2/7
20	3-CF3-4-OMePh	CF3	0.18	0.18	ndd	nd
					nd	nd
21	3-CF3-4-NO2Ph	CF3	0.072	0.072	nd	nd
22	3-CF3-4-NH2Ph	CF3	1.5	3.6	nd	nd
23	3-CF3-4-CNPh	CF3	0.13	0.075	nd	nd
24	3,4-CN2Ph	CF3	0.081	0.14	nd	nd
25	3,4-Cl2Ph	CF3	0.20	0.20	nd	nd

^aF_Survival = proportion of animals living at day 31

^bNES = no extension of survival beyond infected control animals (8 days)

^cEXT = extension of survival beyond infected control animals (8 days), but no survival at day 31

^dnd = not determined