Table 2.
SAR exploration on the nature of the R group: linear alkanes
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Compound | R | FAAHa,b IC50(μM)±SD | COX-1a,b IC50 (μM)±SD | COX-2a,b IC50 (μM)±SD |
10n | ethyl | >100 | 2.1±0.9 | >100 |
10o | n-propyl | >100 | 1.65±0.06 | >100 |
10p | n-butyl | 7.0±1.8 | 0.26±0.07 | >100 |
10q | n-pentyl | 0.57±0.15 | 0.020±0.009 | 0.16±0.02 |
10r, ARN2508 | n-hexyl | 0.031±0.002 | 0.012±0.002 | 0.43±0.02 |
10s | n-heptyl | 0.011±0.003 | 0.37±0.10 | 0.32±0.005 |
10t | n-octyl | 0.003±0.002 | 0.99±0.07 | 28.8±8.4 |
Values are reported as mean values of ≥3 experiments performed
IC50 values were not determined for compounds showing less than 50% inhibition at concentrations of 100 μM for FAAH and COXs.