. Author manuscript; available in PMC: 2017 Jul 14.

Published in final edited form as: J Med Chem. 2016 Jun 24;59(13):6512–6530. doi: 10.1021/acs.jmedchem.6b00719

Table 4.

CQ-sensitive parasite activities for the synthesized mono-, di- and tri-benzamides.

Compound	Derivative info	NF54 parasite IC₅₀ (μM)	D10 parasite IC₅₀ (μM)
12a	Monobenzamides	>41.3 ± ND	ND
12b		5 ± 1	ND
12c		2.3 ± 0.3	2.4 ± ND
12d		5 ± 1	2.3 ±ND
12e		22 ± 4	24 ± 5

15a	R₁ = Nitro	0.7 ± 0.2	0.9 ± 0.1
15b		1.32 ± 0.04	ND
15c		1.4 ± 0.2	ND

15d	R₁ = Cyano	1.9 ± 0.2	2.0 ± 0.2
15e	R₁ = Cyano	ND	5.2 ± ND

15f	R₁ = Methyl	2.5 ± 0.6	ND
15g	R₁ = Methyl	146 ± 1	ND

15h	R₁ = Tert-butyl	1.6 ± 0.2	ND
15i		0.6 ± 0.1	0.7 ± 0.1
15j		8.1 ± 0.5	ND

15k	R₁ = H	9 ± 4	ND
15l	R₁ = H	>314	ND

15m	R₁ = Methoxy	3.0 ± 0.5	ND
15n	R₁ = Methoxy	37 ± 13	ND

15o	R₁ = H (X = N)	>315	ND
15p	R₁ = H (X = N)	>315	ND

20	Tri-phenylbenzamide	81 ± 12	>42

CQ	Standard	0.008 ± 0.002	0.021 ± 0.002