Figure 3.

Correlation of the antischistosomal activity with the inhibition of SmCB1 by azanitrile and carbanitrile analogs. (A) Pairs of analogs with azanitrile and carbanitrile warheads were phenotypically screened against S. mansoni newly transformed schistosomula (NTS) and the data arising was compared to those for the inhibition of SmCB1. Phenotypic changes in the parasite (Table S3) were observed every day for 4 days in the presence of 10 μM inhibitor. Changes were converted to a severity score on a scale from 0 (no effect) to 4 (severe; red heat map). K_i values for SmCB1 inhibition (from Table 1) are shown in the blue heat map. (B) An example of an inhibitor-induced degenerated phenotype in NTS of S. mansoni versus untreated controls (for details, see Table S3).