TABLE 1.

Structures of compounds prepared; inhibition of recombinant SQS for compounds of series 1 and series 2; activities against L. mexicana promastigotes, axenic L. donovani amastigotes, and L-6 cells; and effects on the sterol compositions of L. mexicana promastigotes^a

^aNI, no inhibition, with MIC >10 μM; NE, no effect on sterol composition compared to that for control at the concentration stated; E, effect on sterol composition at the concentration stated, where an effect is considered if there is a change in cholesterol levels of greater than 10 percentage points. Control compounds were miltefosin (IC₅₀ = 0.338 μM) for L. donovani and podophyllotoxin (IC₅₀ = 0.014 μM) for L-6 cells. The IC₅₀s for human SQS were not determined.