Table 5
Affinity and reversibility of lactam inhibitors of PON1 type Q arylesterase activity
| Inhibitor | Structure | Percent Reversibility5-a | IC505-b |
|---|---|---|---|
| % | μM | ||
| Oxindole |
| 100 | 50 |
| Isatin | 20 | NA | |
| 3,4-Dihydro-2(1H)-quinoline | 100 | <25 | |
| 2-Hydroxyquinoline | 100 | <5 | |
| δ-Valerolactam | 100 | 500 | |
| ɛ-Caprolactam | 100 | 100 | |
| N-Bromo-ɛ-caprolactam | 5 | NA |
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↵5-a Percent reversibility determined from percent recovery of purified PON1 type Q arylesterase activity of samples preincubated with lactam, which was then removed by Centricon wash.
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↵5-b Approximate IC50 values determined by titrating inhibition of PON1 type Q arylesterase activity and recording lactam concentrations at which 50% inhibition was observed.