59663-70-6Relevant articles and documents
GABA-uptake inhibitors: Construction of a general pharmacophore model and successful prediction of a new representative
N'Goka,Schlewer,Linget,Chambon,Wermuth
, p. 2547 - 2557 (2007/10/02)
A model for the pharmacophore of GABA-uptake inhibitors was established using published structure-activity data and molecular modeling. The model accounted for the activities of different classes of GABA-uptake inhibitors. Analogues of guvacine substituted at position 6 were synthesized in order to confirm the model. 6-(3,3-Diphenylpropyl)guvacine (30f), which fit well with the pharmacophore, had an in vitro IC50 of 0.1 μM. This value is as good as those of the best GABA-uptake inhibitors known today.
