Table 7.
Examples of 4-(4-cyano-2-thionyl)dihydropyrimidones developed by Bayer HealthCare AG.
|
||||
|---|---|---|---|---|
| Compoundb | R4 | R3 | IC50 (nM)a | Reference |
| 62 | SO2CH3 | H | 0.5 | [157] |
| 63 | SO2CH3 |
|
< 0.3 | [157] |
| 64 | SO2CH3 | SO2CH3 | < 0.3 | [157] |
| BAY 858501 | SO2CH3 | CH3 | < 0.3 | [129,130,157] |
| 65 | SO2CH3 |
|
< 0.3 | [157] |
| 66 | SO2CH3 | CH2CN | < 0.3 | [157] |
| 67 | SO2Ph | H | < 0.3 | [157] |
The results are means of two independent experiments, each performed in duplicate (HNE enzyme assay).
The absolute configuration (S) has been unambiguously assigned by X-ray structure analysis.