Journal of Medicinal Chemistry p. 196 - 202 (1990)
Update date:2022-08-04
Topics:
Kelley, James L.
McLean, Ed W.
Linn, James A.
Krochmal, Mark P.
Ferris, Robert M.
Howard, James L.
A series of 8-substituted analogues of 9-(3-aminobenzyl)-6-(dimethylamino)-9H-purine (8) were synthesized and tested for their ability to bind to the benzodiazepine receptor (BZR) in rat brain tissue.The most active compound was the 8-bromo-9-(3-formamidobenzyl) analogue 16 (IC50 = 0.011 μM), which was 1000-fold more active than the parent 9-benzyl-6-(dimethylamino)-9H-purine (1) and nearly as active as diazepam.Although substitution of a m-formamido group and an 8-bromo substituent on 1 imparted potent BZR binding activity, neither 16 nor 17 analogues exhibited significant anxiolytic activity on a modified Geller-Seifter conflict schedule.
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