Open AccessSynthesis and Structure–Activity Relationship Studies of Conformationally Flexible Tetrahydroisoquinolinyl Triazole Carboxamide and Triazole Substituted Benzamide Analogues as σ2 Receptor Ligands
Author(s) -
Su-Ping Bai,
Shihong Li,
Jinbin Xu,
Xin Peng,
Kiran Kumar Solingapuram Sai,
Wenhua Chu,
Zhude Tu,
Chenbo Zeng,
Robert H. Mach
Publication year - 2014
Publication title -
journal of medicinal chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.01
H-Index - 261
eISSN - 1520-4804
pISSN - 0022-2623
DOI - 10.1021/jm5001453
Subject(s) - benzamide , chemistry , carboxamide , triazole , stereochemistry , receptor , selectivity , 1,2,3 triazole , chemical synthesis , 1,2,4 triazole , structure–activity relationship , combinatorial chemistry , in vitro , biochemistry , medicinal chemistry , organic chemistry , catalysis
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.