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Design, Synthesis, and Biological Evaluation of 8-Phenyl-THIQ as Antidepressive Agents
Xiaopeng Wei1, Fan Yang1, Nuo Xu1
1Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmacy, Tianjin Medical University, Tianjin, P. R. China.
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.
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