Table 1.
Radical scavenging activity and biological properties of the RIV-IND hybrids as well as other reference compounds for comparison.
| Compound | n | R1 | R2 | Antioxidant Activity a
EC50 (µM) |
AChE Inhib b
IC50 (µM) |
BChE Inhib b
IC50 (µM) |
SI c | Aβ42 Self-Aggreg. Inhib d (%) |
|---|---|---|---|---|---|---|---|---|
| 5a1 | 0 | H | H | >2000 | (18 ± 2) × 10 | 29.9 ± 0.4 | 6.0 | 26.9 |
| 5a2 | 0 | OH | H | 8.4 ± 0.2 | 206 ± 4 | 3.22 ± 0.02 | 64.0 | 25.0 |
| 5a3 | 0 | H | OH | 14.5 ± 0.5 | 10.9 ± 0.1 | 10.4 ± 0.4 | 1.05 | 50.3 |
| 5b1 | 1 | H | H | >2000 | 78.4± 0.8 | 8.3 ± 0.1 | 9.4 | 19.9 |
| 5b2 | 1 | OH | H | 7.8 ± 0.5 | 80 ± 2 | 27.1 ± 0.1 | 3.0 | 29.4 |
| 5b3 | 1 | H | OH | 20.2 ± 0.4 | 80.7 ± 0.4 | 5.7 ± 0.3 | 14.2 | 47.8 |
| 5c1 | 2 | H | H | >2000 | 40 ± 2 | 14.5 ± 0.7 | 2.8 | 25.6 |
| 5c2 | 2 | OH | H | 8.5 ± 0.6 | 58.6 ± 0.3 | 15.2 ± 0.4 | 3.8 | 49.9 |
| 5c3 | 2 | H | OH | 20.7 ± 0.4 | 26.8 ± 0.3 | 14.9 ± 0.7 | 1.8 | 55.5 |
| Deferiprone | - | - | - | 148 ± 3 | - | - | ||
| Trolox | - | - | - | 13.8 ± 0.2 | - | - | ||
| Rivastigmine e | - | - | - | - | 32.1 | 0.39 | 82.3 | |
| Curcumin e | - | - | - | - | - | - | - | 65.7 |
a Radical scavenging activity (DPPH method), with mean values of three independent experiments; b mean values of two independent experiments ± SD, performed with eeAChE and eqBChE; c selectivity index = IC50 (AChE)/IC50 (BChE); d mean values of two independent measurements in duplicate (SEM < 10%) for inhibition of Aβ42 aggregation (Cinhibitor = 20 µM) (thioflavin T fluorescence method); e Ref. [24].