Table 3. Inhibition of SmCB1 and Antischistosomal Activity of Azadipeptide Nitriles.

^aCompounds 1a to 7a are also presented in Table 1.

^bThe abbreviations used are as follows:

^cThe K_i values were determined using a kinetic activity assay with the fluorogenic peptide substrate Cbz-Phe-Arg-AMC.

^dPhenotypic changes in the parasite in the presence of 10 μM inhibitor are indicated for 24 and 48 h (see Table S3) and converted to a severity score on a scale from 0 (no effect) to 4 (severe).

^e2a is listed in both P1 and P2 sections.

^fN-Methylated leucine.