Synthesis and Structure–Activity Relationship Studies of Conformationally Flexible Tetrahydroisoquinolinyl Triazole Carboxamide and Triazole Substituted Benzamide Analogues as σ2Receptor Ligands
Journal of Medicinal Chemistry2014Vol. 57(10), pp. 4239–4251
Citations Over TimeTop 17% of 2014 papers
Su‐Ping Bai, Shihong Li, Jinbin Xu, Xin Peng, Kiran Kumar Solingapuram Sai, Wenhua Chu, Zhude Tu, Chenbo Zeng, Robert H. Mach
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 (11)C-labeled versions of these compounds may be potential σ2-selective radiotracers for imaging the proliferative status of solid tumors.
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