Table 2. Profile of Analogues 4–13, with Substitutions and Nitrogen Insertions on the Central Phenyl Ring.

^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.

^bAqueous 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.