Table 1.
Relative Inhibition of Human BHMT by Compounds 1 and 5–21a
| Compound | % Inhibitionb (average of triplicates) (0.25 mM betaine, 0.1 mM dl-homocysteine) |
IC50(μM)±SEMc (n = 3) (2 mM betaine, 1 mM dl-homocysteine) |
||
|---|---|---|---|---|
| 20 μM | 1 μM | |||
| 1 |  |
100.0 | 97.6 | 0.138±0.019 |
| Series 1 | ||||
| 5 |  |
19.1 | Nd | Nd |
| 6 |  |
97.6 | 26.3 | 3.26±0.59 |
| 7 |  |
5.4 | Nd | Nd |
| 8 |  |
9.8 | Nd | Nd |
| 9 |  |
100.0 | 94.3 | 0.649±0.103 |
| 10 |  |
2.11 | Nd | Nd |
| Series 2 | ||||
| 11 |  |
0.0 | 0.0 | Nd |
| 12 |  |
23.8 | 5.1 | Nd |
| 13 |  |
98.5 | 58.9 | 2.50±0.19 |
| 14 |  |
19.8 | Nd | Nd |
| 15 |  |
15.5 | Nd | Nd |
| 16 |  |
37.1 | Nd | Nd |
| 17 |  |
0.0 | Nd | Nd |
| 18 |  |
3.3 | 0.0 | Nd |
| 19 |  |
79.01 | 22.4 | Nd |
| 20 |  |
100.0 | 97.8 | 0.139±0.012 |
| 21 |  |
100.0 | 98.1 | 0.084±0.004 |
a
The percent inhibition of each compound was determined at 20 and 1 μM. See the Experimental Section for details.
b
All assays were done in triplicate, and the obtained data were reproducible within ±15%.
c
All data points for IC50 values were derived from assays performed in duplicate, and the values were obtained from 3 different assays. Nd means not determined.