Indoloxypropanolamine analogues as 5-HT1A receptor antagonists

Analogues of pindolol, 1-(1H-indol-4-yloxy)-3-isopropylamino-propan-2-ol, were synthesized and evaluated as 5-HT1A receptor antagonists. The structural features required for optimal binding to the 5-HT1A receptor are as follows: S-2-propanol linker, 4-indoloxy substituent, and a large lipophilic cyclic amine substituent.

The discovery and synthesis of the 5-HT1A receptor antagonist 13a is reported.Figure optionsDownload as PowerPoint slide