Table 4 The pharmacokinetic properties of the compounds BZ1 and BZ1-I, based on human microsome studies, revealing their metabolic stability and clearance potential

From: Identification of potent inhibitors of Leishmania donovani and Leishmania infantum chagasi, the causative agents of Old and New World visceral leishmaniasis

Parameter

BZ1

BZ1-I

Remarks

T1/2 (min)

47

57

Both compounds exhibited moderate metabolic stability.

CLint, in vitro (μL/min/mg protein)

37

31

Comparable in vitro clearance rates, indicating manageable metabolism.

Predicted CLint, in vivo (mL/min/kg)

30

25

BZ1-I showed slightly lower intrinsic clearance, favouring longer half-life.

Predicted CLblood (mL/min/kg)

12

11

Both compounds demonstrated moderate blood clearance, enhancing systemic exposure.

Predicted extraction ratio (EH)

0.59

0.55

Moderate EH values align with intermediate clearance classifications.

Clearance classification

Intermediate

Intermediate

Suitable for further optimization but not optimal for high-clearance pathways.

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