Table 1.
IC50 values for selected peptidomimetics against S. aureus AgrC in groups I–IV.[a]
| Inhibitor | Group I | IC50 [nm][b] | Group IV | |
|---|---|---|---|---|
| Group II | Group III | |||
| t-AIP-II[c] | 260 (95–695) | 230 (190–270) | 4 (3–5) | 150 (90–260) |
| t-AIP-II[d] | 101 (88–117) | 97 (94–112) | 9.3 (7.7–11.4) | 140 (118–166) |
| n7FF | 340 (308–376) | 495 (435–564) | 34.8 (30.8–39.4) | 985 (825–1176) |
| n8FF | 468 (422–518) | 479 (410–559) | 125 (109–142) | 3486 (2301–5280) |
| n7OFF | 181 (154–213) | 583 (468–725) | 332 (280–395) | 5938 (4221–8352) |
| n7FF amide | 3935 (3593–4309) | 2200 (1727–2801) | 573 (472–696) | –[e] |
| n8FF amide | 4742 (4335–5187) | 1339 (1065–1683) | 2613 (2180–3131) | –[e] |
| n7OFF amide | –[f] | –[f] | –[f] | –[f] |
[a]
See Experimental Section for details of strains and assay protocols.
[b]
95 % confidence interval provided in parentheses.
[c]
Values reproduced from ref. [5l] with different S. aureus reporter strains.
[d]
Values differ slightly in groups III and IV from those previously reported in ref. [4k] due to day-to-day assay variations.
[e]
Data not shown due to non-sigmoidal curves in group IV, with maximal inhibition not reached at the highest concentration tested.
[f]
Inactive over the concentrations tested.