TABLE 1.

Representative classes of sortase inhibitors revealed by HTS

		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.