Table 2.

In vitro antileishmanial activity and CYP inhibition of antifungal azoles and non-azole compounds

Compound	EC50 or IC50 (μM)			SIc
	EC50 (L. donovani)a	IC50 (LdCYP51)b	IC50 (LdCYP5122A1)b
Imidazole
Bifonazole	12 ± 1	0.057 ± 0.008	0.33 ± 0.07	5.7
Butoconazole	1.9 ± 0.4	0.073 ± 0.008	0.32 ± 0.07	4.4
Clotrimazole	5.0 ± 0.1	0.068 ± 0.004	0.26 ± 0.08	3.8
Econazole	9.4 ± 0.3	0.046 ± 0.004	0.47 ± 0.13	10
Fenticonazole	5.6 ± 0.3	0.081 ± 0.002	0.65 ± 0.08	8.0
Isoconazole	6.2 ± 0.5	0.049 ± 0.003	0.43 ± 0.04	8.8
Ketoconazole	22 ± 6	0.048 ± 0.007	0.42 ± 0.05	8.7
Miconazole	7.6 ± 0.7	0.057 ± 0.003	1.1 ± 0.2	19
Oxiconazole	3.9 ± 0.4	0.032 ± 0.002	0.62 ± 0.02	20
Sertaconazole	7.1 ± 0.5	0.064 ± 0.007	1.1 ± 0.2	17
Sulconazole	7.4 ± 0.6	0.064 ± 0.003	0.38 ± 0.06	5.9
Tioconazole	9.5 ± 0.6	0.054 ± 0.008	1.1 ± 0.2	20
Triazole
Efinaconazole	15 ± 1	0.068 ± 0.002	6.2 ± 1.7	92
Fluconazole	>100d	0.96 ± 0.05	>100	>105
Isavuconazole	12 ± 0	0.043 ± 0.007	2.6 ± 0.7	60
Itraconazole	6.0 ± 1.1	0.049 ± 0.009	2.1 ± 0.4	43
Posaconazole	2.8d	0.059 ± 0.003	1.5 ± 0.3	25
Ravuconazole	12 ± 2	0.049 ± 0.008	12 ± 4	248
Terconazole	13 ± 1	0.083 ± 0.009	12 ± 3	140
Voriconazole	>100	0.085 ± 0.017	>100	>1176
Non azole compounds
Miltefosine	2.7e	12 ± 1	43 ± 1	3.5
Pentamidine	14 ± 1	No inhibition at 100 μM	No inhibition at 100 μM	NA
Paromomycin	>50e	No inhibition at 100 μM	No inhibition at 100 μM	NA
Amphotericin B	0.14 ± 0.01	<25% inhibition at 10 μM	<25% inhibition at 10 μM	NA
DB766	0.036f	<30% inhibition at 30 μM	1.0 ± 0.1	<0.035

^a Mean ± standard deviation (n ≥ 3).

^bMean ± standard deviation (n = 3).

^cSI (selectivity index) = IC₅₀ against LdCYP5122A1/IC₅₀ against LdCYP51.

^dPublished data from Feng et al. (ref. ¹⁸).

^eIC₅₀ vs. intracellular amastigotes from Wang et al. (ref. ⁴⁵).

^fIC₅₀ vs. intracellular amastigotes from Wang et al. (ref. ⁴⁵), see also Fig. 7.

Source data are provided as a Source Data file.