Design, Synthesis, and Biological Evaluation of 8-Phenyl-THIQ as Antidepressive Agents

Drug Dev Res. 2025 Sep;86(6):e70156. doi: 10.1002/ddr.70156.

ABSTRACT

The structural modification and derivatization of natural products represent an essential pathway for pharmaceutical innovation in the management of depression. The 8-phenyl tetrahydroisoquinoline, as a parent core, was obtained from magnoflorine by a structural simplification strategy. The present report details the synthesis and antidepressant activity studies of 8-phenyl-THIQ analogs. Among them, compounds 1e and 1j exhibited significant antidepressant activity in addition to high synthetic accessibility and adequate predictive ADME/T properties.

PMID:40919677 | DOI:10.1002/ddr.70156