Selective inhibition of PfA-M1, over PfA-M17, by an amino-benzosuberone derivative blocks malaria parasites development in vitro and in vivo

Table 1 Summary of in vitro and in vivo PfA-M1 inhibitors properties

	Ki rPfA M1 (nM)	Ki rPfA M17 (nM)	IC₅₀ in vitro (µM)	In vitro strain	In vivo model	In vivo parasitaemia reduction (%)	References
CHR-2863	1413.41 ± 123.74	75.96 ± 22.86	0.37	3D7	P. c. chabaudi/C57/BL6j	43% (25 mg/kg)	[46]
			0.376	K1		43% (25 mg/kg)
						52% (50 mg/kg)
						66% (100–50 mg/kg)
Bestatin	1673.00 ± 238.05	613 ± 201.33	5	3D7	P. c. chabaudi/8 weeks old C57/BL6j	34% at 100 mg/kg, twice a day	[46, 47]
		613 ± 201.33	12–21	Dd2
		25 ± 1.2	11–15	D10
		25 ± 1.2	8–14	3D7
Malarone	NA	NA	–	–	P. c. chabaudi/C57/BL6j	100% at 14 mg/kg	[46]
Chloroquine	–	–	10.1 ± 3.8	3D7	P. c. chabaudi/8 weeks old C57BL/6j	85% at 5 mg/kg	[47]
Chloroquine	–	–	138.0 ± 21.1	FcB1	P. c. chabaudi/8 weeks old C57BL/6j	85% at 5 mg/kg	[47]
Compound 4	79	13.2 ± 0.5	20–40	Dd2	P. c. chabaudi/8 weeks old C57BL/6j	92% at 100 mg/kg, twice a day	[31, 47]
			46–75	D10
			24–62	3D7
T5	50	> 100 µM	11.2 ± 3.4	3D7	P. c. chabaudi/BALB/c	44 and 40% at 12 and 24 mg/kg/day	this work
T5	50	> 100 µM	6.5 ± 2.4	FcB1	P. c. chabaudi/BALB/c	44 and 40% at 12 and 24 mg/kg/day	this work

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