122479-46-3Relevant academic research and scientific papers
Imidazopyridazines. VIII. Syntheses and Central Nervous System Activities of Some 6-Benzylamino(and methoxybenzylamino)-3-methoxy-2-phenyl(substituted phenyl or pyridinyl)imidazopyridazines
Barlin, Gordon B.,Davies, Les P.,Ngu, Maria M. L.
, p. 1759 - 1768 (2007/10/02)
Syntheses and IC50 values for the displacement of 3H-diazepam from rat brain plasma membrane are reported for a series of 6-benzylamino(and methoxybenzylamino)-3-methoxy-2-phenyl(substituted phenyl and pyridinyl)imidazopyridazines (and their 6-anilino and 6-phenethylamino analogues).The results are compared with those reported previously (by us) for the 6-chloro, 6-phenoxy, 6-benzylthio, and 6-benzyloxy compounds.In the imidazopyridazine ring system, 6-(o- and m-methoxybenzylamino) groups were found to be beneficial to binding activity; eight compounds have been prepared with IC50 values less than 2 nM (cf. 3H-diazepam with IC50 of 4.2 nM). 2-(p-Aminophenyl)-3-methoxy-6-(m-methoxybenzylamino)imidazopyridazine exhibited the highest activity with IC50 1.0 nM.
