Table 5. Effect of Scaffold Hops on Activity and Physicochemical Properties.

^aData reported previously for 1 and 24.¹⁰

^bINMAC 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.

^cAqueous solubility is the kinetic solubility measured by CLND.

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

^eCl_i is the mouse liver microsomal intrinsic clearance.

^fND means not determined.