Table 2.
Biological data of 4-alkoxyphenylglycinamides
 | |||
|---|---|---|---|
| Compound | R | cAMP pEC50 (EC50, nM)a | Emaxb |
| 4 | 6.21 ± 0.08 (616) | 97 ± 4 | |
| 30 | H | 6.24 ± 0.07 (575) | 97 ± 7 |
| 31 | Methyl | 6.53 ± 0.08 (295) | 116 ± 4 |
| 32 | Ethyl | 6.92 ± 0.11 (120) | 99 ± 4c |
| 33 | n-Propyl | 6.40 ± 0.04 (398) | 113 ± 8 |
| 34 | i-Propyl | 6.74 ± 0.04 (182) | 102 ± 3 |
| 35 | t-Butyl | 6.50 ± 0.01 (316) | 109 ± 10c |
| 36 | Butan-2-yl | 6.61 ± 0.04 (245) | 96 ± 3 |
| 37 | 3-Methylbutan-2-yl | 6.67 ± 0.07 (214) | 93 ± 6c |
| 38 | Cyclopropyl | 6.62 ± 0.04 (240) | 98 ± 4 |
| 39 | Cyclopropylmethyl | 6.68 ± 0.09 (209) | 94 ± 4c |
| 40 | Cyclobutyl | 6.55 ± 0.04 (282) | 98 ± 2 |
| 41 | 1-Methylcyclobutyl | 6.63 ± 0.04 (234) | 91 ± 4c |
| 42 | Cyclopentyl | 6.68 ± 0.01 (209) | 107 ± 4c |
| 43 | Cyclohexyl | 6.25 ± 0.07 (562) | 83 ± 2c |
| 44 | MeOOCCH2 | 6.33 ± 0.05 (468) | 103 ± 8 |
| 45 | HOCH2CH2 | 6.37 ± 0.12 (427) | 99 ± 4 |
| 46 | MeOCH2CH2 | 6.27 ± 0.02 (537) | 107 ± 11 |
| 47 |  |
6.33 ± 0.04 (468) | 110 ± 1c |
| 48 | BocNHCH2CH2 | 6.05 ± 0.07 (891) | 97 ± 7c |
| 49 | NH2CH2CH2 | 5.10 ± 0.05 (7943) | 129 ± 4c |
| 50 | MeN(Boc)CH2CH2 | 6.29 ± 0.03 (513) | 111 ± 1c |
| 51 | MeNHCH2CH2 | 5.26 ± 0.06 (5495) | 122 ± 4c |
| 52 | Me2NCH2CH2 | 5.26 ± 0.06 (5495) | 103 ± 4c |
| 53 |  |
5.47 ± 0.07 (3388) | 120 ± 5c |
| 54 |  |
<5.00 | N.D. |
a
pEC50 values are means ± standard error of at least three independent experiments performed in duplicate.
b
Emax value is % of 2-PCCA (mean ± standard error).
c
Emax value is % of RTI-13951-33 (mean ± standard error).
N.D., Not determined.