Table 1. Structure and Activities of Compounds 7–20 Evaluated by an Enzymatic Assay.
Inh %: inhibition percentage at 100 μM concentration.
IC50: measured in μM by an enzymatic assay from an average of three experiments. IC50 values were determined for compounds that showed >90% inhibition at 100 μM.
LE was calculated using the equation: LE = (1.37 × pIC50)/HA, where HA means heavy atom, i.e., a non-hydrogen atom. LE: compound 14 = 0.29; compound 19 = 0.31.