Table 6. Effect of Modifications or Replacements to the Morpholine Group on Activity and Physicochemical Properties.

^aINMAC is the intramacrophage assay carried out in THP-1 cells with L. donovani amastigotes. Data are the result of at least three independent replicates and standard deviations are ≤0.4.

^bAq. solubility is the kinetic solubility measured by CLND.

^cFaSSIF solubility is the fasted state simulated intestinal fluid solubility.

^dCl_i is the mouse liver microsomal intrinsic clearance.

^eData reported previously.¹⁰

^fND means not determined.