In vitro and in vivo characterization of anti-malarial acylphenoxazine derivatives prepared from basic blue 3

Malaria Journal

Table 1 Anti-malarial activity of basic blue 3 and ITT derivatives in vitro

	3D7	W2	MRA-1239	MRA-1240
	IC₅₀ (nM)^a	IC₅₀ (nM)^a	IC₅₀ (nM)^a	IC₅₀ (nM)^a
basic blue 3	3.2 ± 0.19	4.8 ± 0.53	5.2 ± 1.1	5.9 ± 0.68
ITT-001	11.2 ± 1.3	11.1 ± 1.8	34.6 ± 9.1	39.0 ± 11.2
ITT-002	10.7 ± 1.5	10.4 ± 2.8	20.7 ± 1.6	24.4 ± 3.7
ITT-003	9.8 ± 1.0	9.6 ± 2.1	24.9 ± 3.1	31.3 ± 9.8
ITT-004	11.3 ± 2.4	12.3 ± 2.7	26.4 ± 2.9	30.5 ± 2.0
ITT-005	138.3 ± 9.0	145.6 ± 29.5	130.2 ± 9.3	183.7 ± 30.1
ITT-006	10.6 ± 1.6	16.0 ± 4.5	27.5 ± 3.4	29.4 ± 5.8
CQ	8.6 ± 0.21	225.0 ± 23.2***	38.6 ± 5.2	58.0 ± 2.6*
ART	ND	ND	5.5 ± 0.018	13.2 ± 1.4**

IC₅₀ concentration of 50% inhibition of parasite growth, SEM standard error of the mean, CQ chloroquine, ART artemisinin, ND not determine
IC_50s were compared between 3D7 and W2 strains and between MRA-1239 and MRA-1240 isolates (two-tailed unpaired Student’s t-test: * P < 0.05; ** P < 0.01; and *** P < 0.001)
^aData represent the mean ± SEM values for three experiments

ISSN: 1475-2875