Table 2.
Entry | R– | Inhibition at 1 mM (%) | IC50 (μM) | Ki (μM) |
---|---|---|---|---|
1 1 | * CH3OCH2CH2– | 83 | 31 | 13 |
2 1 | CH3NHCH2CH2– | 29 | - | - |
3 1 | (CH3)2NHCH2CH2– | 14 | - | - |
4 1 | CH3SHCH2CH2– | 80 | 408 | - |
5 1 | FCH2CH2– | 67 | 379 | - |
6 1 | BnCH2– | 55 | 866 | - |
7 2 | CH3CH2CH2– | 60 | 283 | 90 |
8 2 | CH2CHCH2– | 70 | 207 | 58 |
9 2 | CH2CHCH2CH2– | 71 | 189 | 57 |
10 2 | CHCCH2– | 83 | 55 | 17 |
11 2 | F3CCH2– | 41 | - | - |
12 2 | O2N– | 6 | - | - |
13 2 | NH2COCH2CH2– | 43 | - | - |
* Denotes L-257 (39) (Scheme 9); 1 Measured by Ultra Performance Liquid Chromatography-Mass Spectrometry; 2 Measured by colorimetric assay.