Synthesis and Structure–Activity Relationship Studies of Conformationally Flexible Tetrahydroisoquinolinyl Triazole Carboxamide and Triazole Substituted Benzamide …

…, J Xu, X Peng, K Sai, W Chu, Z Tu, C Zeng…

Index: Bai, Suping; Li, Shihong; Xu, Jinbin; Peng, Xin; Sai, Kiran; Chu, Wenhua; Tu, Zhude; Zeng, Chenbo; Mach, Robert H. Journal of Medicinal Chemistry, 2014 , vol. 57, # 10 p. 4239 - 4251

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Citation Number: 5

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.