Table 1.
Inhibitory activity of pyrrolidines 2–5 against the class II α-mannosidases GMIIb, LManII and JBMan from GH38 family enzymes.
Compound | GMIIb [IC50 (M)] |
LmanII [IC50 (M)] |
JBMana (%) |
1a [30] | (8.8 ± 0.06) × 10−5 | 7.0 × 10−3 | 1 |
2a | (3.6 ± 0.20) × 10−4 | n.i.a | n.i. |
2b | (3.5 ± 0.17) × 10−4 | n.i.a | n.i. |
2c | (3.0 ± 0.18) × 10−4 | n.i.a | n.i. |
3a | (7.5 ± 0.35) × 10−4 | n.i.a | 3 |
3b | (9.5 ± 0.33) × 10−4 | n.i.a | 14 |
3c | (4.5 ± 0.14) × 10−4 | n.i.a | 39 |
4a | (18.0 ± 0.40) × 10−4 | n.i.a | 2 |
4b | (16.0 ± 0.40) × 10−4 | n.i.a | 4 |
4c | (19.0 ± 0.46) × 10−4 | n.i.a | 17 |
5a | (19.5 ± 0.41) × 10−4 | n.i.a | 21 |
5b | (26.5 ± 0.51) × 10−4 | n.i.a | 40 |
5c | (29.5± 0.56) × 10−4 | n.i.a | 38 |
aInhibition in the presence of 2 mM inhibitor concentration; n.i. no inhibition.