Synthesis and dopamine receptor binding studies of homochiral 8-aminopyrido[1,2-a]indoles.
نویسندگان
چکیده
Starting from L-aspartic acid the preparation of 8-aminopyrido[1,2-a]indole derivatives as benzo-fused analogs of the dopamine autoreceptor agonist 1 is reported. The key step of the synthesis is the Tf2O induced cyclization of the 1,2-amino alcohol 6. Receptor binding studies indicated selective affinity for the D-2 autoreceptor. Among the tested compounds, the dipropylamino derivative 2 showed the highest affinity for the D-2 receptor labelled with the selective autoreceptor agonist pramipexole (IC50 value: 450 nM). Thus, 2 is 15 times less potent than the aminoindolizine 1.
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ورودعنوان ژورنال:
- Archiv der Pharmazie
دوره 328 7-8 شماره
صفحات -
تاریخ انتشار 1995