Table 4.
Biological data of bioisosteric 1,3,4-oxadiazoles
 | |||||
|---|---|---|---|---|---|
| Compound | Structure | R | clog Pa | cAMP pEC50 (EC50, nM)b | Emaxc |
| 71 | A |  |
4.26 | 6.27 ± 0.01 (537) | 103 ± 5d |
| 72 | A |  |
4.39 | 6.28 ± 0.06 (525) | 101 ± 5d |
| 73 | B |  |
3.35 | 6.32 ± 0.09 (479) | 94 ± 0 |
| 74 | B |  |
3.48 | 6.26 ± 0.06 (550) | 96 ± 4 |
| 82 | A |  |
4.35 | 6.95 ± 0.10 (112) | 96 ± 4 |
| 83 | A |  |
4.47 | 6.83 ± 0.08 (148) | 95 ± 3 |
| 84e | A |  |
4.20 | 7.23 ± 0.03 (59) | 99 ± 0 |
| 85 | B |  |
3.56 | 6.53 ± 0.03 (295) | 104 ± 3 |
| 86 | B |  |
3.44 | 6.43 ± 0.01 (372) | 98 ± 3 |
| 87e | B |  |
3.29 | 6.86 ± 0.01 (138) | 92 ± 9 |
| 88e | C |  |
4.20 | 7.11 ± 0.02 (78) | 97 ± 3 |
| 89e | D |  |
4.20 | 7.13 ± 0.08 (74) | 103 ± 3 |
| 90e | E |  |
3.76 | 7.15 ± 0.08 (71) | 101 ± 1 |
| 91e | F |  |
3.76 | 6.86 ± 0.04 (138) | 107 ± 2 |
a
clog P was calculated using Instant JChem 5.4.0 (ChemAxon Ltd.).
b
pEC50 values are means ± standard error of at least three independent experiments performed in duplicate.
c
Emax value is % of RTI-13951-33 (mean ± standard error).
d
Emax value is % of 2-PCCA (mean ± standard error).
e
Compounds were tested as the HCl salt.