TABLE 1.

In vitro antileishmanial activities of AIAs and their physicochemical properties

Compound	IC50 (μM)a vs:					pKa	Log P	LogD7.4	ΔTm(AT)e
	L. donovani axenic amastigotes	L. donovani LV82 intracellular amastigotes	L. amazonensis intracellular amastigotes	L. major intracellular amastigotes	Murine peritoneal macrophages
DB745	0.50 ± 0.15	0.018 ± 0.007	0.12 ± 0.02	0.026 ± 0.011	4.5 ± 1.4	7.12	3.82	3.63	7.1
DB766	0.50 ± 0.10	0.036 ± 0.005	0.087 ± 0.015	0.014 ± 0.004	2.8 ± 0.8	7.36	4.41	4.12	6.0
Amphotericin B	0.098 ± 0.013	0.066 ± 0.012	0.14 ± 0.01	0.21 ± 0.05	8.2 ± 1.1	ND	ND	ND	ND
Miltefosine	8.5 ± 1.2	2.7 ± 0.3	15 ± 3	25 ± 3	24 ± 15b	ND	ND	ND	ND
Paromomycin	>50	>50	19 ± 3	25 ± 2	>100	ND	ND	ND	ND
Pentamidine	1.8 ± 0.4	>50d	0.83 ± 0.17	NDc	14 ± 5	11.6	1.7	<−2.0	12.8f

^aMean ± standard error of at least three independent determinations unless noted otherwise.

^bMean ± range of two independent determinations.

^cND, not determined.

^dPentamidine is known to reduce the number of parasites per macrophage in in vitro experiments but not the number of infected macrophages as assessed here.

^eIncrease in DNA thermal melting of poly(dA-dT).

^fSee work by Stephens et al. (27).