Synthesis and Structure–Activity Relationship Studies of Conformationally Flexible Tetrahydroisoquinolinyl Triazole Carboxamide and Triazole Substituted Benzamide Analogues as σ2Receptor Ligands
Year: 2014
Type: article
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.
Source: Journal of Medicinal Chemistry
DOI: 10.1021/jm5001453
Institutions: Washington University in St. Louis, Henan Medical University
Language: English
Subfield: Molecular Biology
Domain: Life Sciences
Open Access status: green
Awards: G2495129529, G423073863, G967493355
OpenAlex ID: W2328952638