TABLE 1
Structure-activity relationships
| ||||||||||
| Compound | R2 | R3 | R4 | R5 | IC50 | |||||
| μM | ||||||||||
| CNTinh-01 | 3-bicyclo[2.2.1]heptyl-2-carboxylic acid | OMe | 2-Cl-phenyl | H | 15 | |||||
| CNTinh-02 | 3-bicyclo[2.2.1]heptyl-2-carboxylic acid | OMe | 3,4-dimethyl-phenyl | Me | 4 | |||||
| endo-CNTinh-03 | 3-bicyclo[2.2.1]heptyl-2-carboxylic acid | OMe | 4-methyl-phenyl | Me | 4 | |||||
| endo-CNTinh-04 | 3-bicyclo[2.2.1]heptyl-2-carboxylic acid | OEt | 4-Cl-phenyl | Me | 6 | |||||
| exo-CNTinh-03 | 3-bicyclo[2.2.1]heptyl-2-carboxylic acid | OMe | 4-methyl-phenyl | Me | 4 | |||||
| exo-CNTinh-04 | 3-bicyclo[2.2.1]heptyl-2-carboxylic acid | OEt | 4-Cl-phenyl | Me | 6 | |||||
| CNTinh-05 | 3-bicyclo[2.2.1]heptyl-2-carboxylic acid | OEt | 3,4-dimethyl-phenyl | Me | 6 | |||||