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Inhibitory and chaperone activity of various N-alkyl conduramine F-4 against wild-type and mutant human β-galactosidase
| R | IC50 (µM) against wild type | Enhanced activity (fold) of the R201C mutant with N-alkyl-conduramine F-4 derivatives (20 µM) | |
|---|---|---|---|
| (a) | n-Butyl | 50 | 2.0 |
| n-Pentyl | 19 | 4.0 | |
| n-Hexyl | 56 | 4.6 | |
| n-Octyl (175) | 120 | 5.4 | |
| n-Decyl | 43 | 1.6 | |
| (b) | (CH2)3OH | >1000 | 0.9 |
| CHEt2 | >1000 | 1.2 | |
| Cy | 490 | 1.4 | |
| (c) | CH2CHEt2 (176) | 15 | 7.4 |
| CH2Cy (28) | 60 | 8.5 | |
| CH2CHMe2 | 41 | 4.6 | |
| CH2Ph | 180 | 1.5 | |
| (CH2)2CHMe2 | 28 | 4.6 | |
| (CH2)2Ph | 86 | 4.2 | |
