Synthesis and structure-activity relationship studies of conformationally flexible tetrahydroisoquinolinyl triazole carboxamide and triazole substituted benzamide analogues as σ2 receptor ligands

Suping Bai, Shihong Li, Jinbin Xu, Xin Peng, Kiran Sai, Wenhua Chu, Zhude Tu, Chenbo Zeng, Robert H. Mach

Research output: Contribution to journalArticlepeer-review

18 Scopus citations

Abstract

Two novel classes of compounds targeting the sigma-2 (σ2) receptor were synthesized, and their bioactivities to binding σ1 and σ2 receptors were measured. Four novel triazole carboxamide analogues, 24d, 24e, 24f, and 39c, demonstrated high affinity and selectivity for the σ2 receptor. These data suggest 11C-labeled versions of these compounds may be potential σ2-selective radiotracers for imaging the proliferative status of solid tumors.

Original languageEnglish
Pages (from-to)4239-4251
Number of pages13
JournalJournal of Medicinal Chemistry
Volume57
Issue number10
DOIs
StatePublished - May 22 2014

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