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. Author manuscript; available in PMC: 2016 Nov 1.
Published in final edited form as: Bioorg Med Chem Lett. 2015 Jun 23;25(21):4834–4837. doi: 10.1016/j.bmcl.2015.06.066

Table 2.

Antitrypanosomal Activity and in vitro ADME properties of selected cruzain inhibitors.

compound MDCK (Papp cm/s * 10−6) CYP 3A4 IC50 (μM) T. cruzi IC50
4 3.02 3.8 0.022
6 3.49 1.2 0.38
8 0.48 0.26 0.015
11 2.26 0.3 0.037
16 6.8 0.20 0.01
20 15.1 0.314 0.01
21 2.9 0.263 0.003
a

Permeability (A to B) in MDCK cell monolayers.

b

Inhibition of CYP3A4 in vitro.

c

Antitrypanosomal activity of compounds against intracellular T. cruzi in C2C12 host cells using high-content imaging as described in the text and in ref 18.