Table 1. Effect of Changing Core Structures on Enzyme- and Cell-Based Activitiesb.
Selectivity = IC50 (HsNMT1)/IC50 (LdNMT). LipE = pIC50 – clog P; where values for LdNMT and LmNMT were obtained, the average LipE is reported. EC50 for intracellular L. donovani amastigotes.
Toxicity against bone-marrow-derived macrophages; nAUC, normalized area under the curve. The dose–response curves are shown in Figures S6–S10.