TABLE 1

Structures and activities of benzaldazine analogs Embedded Image

R Allosteric Activity Potency
μM
3,3′-Difluorobenzaldazine 3,3′-F Positive 2.6 ± 0.4
2,2′-Difluorobenzaldazine 2,2′-F Positive 14 ± 12
4,4′-Difluorobenzaldazine 4,4′-F Negative >100
3,3′-Dimethoxybenzaldazine 3,3′-OCH3 Negative 3.0 ± 0.4
4,4′-Dimethoxybenzaldazine 4,4′-OCH3 Negative >100
3,3′-Dichlorobenzaldazine 3,3′-Cl Neutral 7.6 ± 1.9 vs. DFB
Neutral 17 ± 16 vs. DMeOB
3,3′-Dihydroxybenzaldazine 3,3′-OH Neutral >50