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Synthesis and structure-activity relationship studies of conformationally flexible tetrahydroisoquinolinyl triazole carboxamide and triazole substituted benzamide analogues as ?2 receptor ligands.

ABSTRACT: Two novel classes of compounds targeting the sigma-2 (?2) receptor were synthesized, and their bioactivities to binding ?1 and ?2 receptors were measured. Four novel triazole carboxamide analogues, 24d, 24e, 24f, and 39c, demonstrated high affinity and selectivity for the ?2 receptor. These data suggest (11)C-labeled versions of these compounds may be potential ?2-selective radiotracers for imaging the proliferative status of solid tumors.

SUBMITTER: Bai S

PROVIDER: S-EPMC6818095 | biostudies-literature | 2014 May

REPOSITORIES: biostudies-literature

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

Bai Suping S Li Shihong S Xu Jinbin J Peng Xin X Sai Kiran K Chu Wenhua W Tu Zhude Z Zeng Chenbo C Mach Robert H RH

Journal of medicinal chemistry 20140512 10

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. ...[more]

PMID: 24821398

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