TABLE 1.
Percent Inhibition, Range [Median] | ||||
---|---|---|---|---|
Class | Chemotype [Number, of 407] | S. aureus SrtA | B anthracis SrtA | C. papaya papain |
I |
[16] |
44–92 [68] | 71–92 [90] | 0–77 [53] |
II |
[8] |
22–92 [70] | 63–90 [87] | 0–51 [10] |
III |
[6] |
34–92 [71] | 27–85 [38] | 2–53 [21] |
IV |
[18] |
13–92 [66] | 1–91 [78] | 0–40 [14] |
V |
[9] |
27–93 [65] | 19–92 [73] | 0–22 [7] |
Shown are the core structures of five chemotypes of sortase inhibitors with a cluster size ≥6 that demonstrate limited inhibition of papain. The range of percent inhibitions observed for the class and the median (brackets) are shown for sortase A (S. aureus and B. anthracis) and papain (C. papaya). R, R′, and R″ indicate a hydrogen atom or an alkyl-type substituent (alkyl, methylene, or methine); Ar indicates a carbocyclic aromatic or heteroaromatic, including complex arrays; X indicates a heteroatom functional group such as OR, -NHR, etc.; and a dashed line indicates the presence/absence of a ring unsaturation.