- Synthesis and structure-activity relationship studies of conformationally flexible tetrahydroisoquinolinyl triazole carboxamide and triazole substituted benzamide analogues as σ2 receptor ligands
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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.
- Bai, Suping,Li, Shihong,Xu, Jinbin,Peng, Xin,Sai, Kiran,Chu, Wenhua,Tu, Zhude,Zeng, Chenbo,Mach, Robert H.
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supporting information
p. 4239 - 4251
(2014/06/09)
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- An efficient F-18 labeling method for PET study: Huisgen 1,3-dipolar cycloaddition of bioactive substances and F-18-labeled compounds
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The Cu(I)-catalyzed, 1,3-dipolar cycloaddition reaction was applied successfully to the synthesis of small, F-18-labeled biomolecules, and an optimal condition was developed for one-pot, two-step reaction without any interim purifications. This technique was employed in various F-18-labeled, 1,2,3-triazole syntheses with high radiochemical yield.
- Sirion, Uthaiwan,Kim, Hee Jun,Lee, Jae Hak,Seo, Jai Woong,Lee, Byoung Se,Lee, Sang Ju,Oh, Seung Jun,Chi, Dae Yoon
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p. 3953 - 3957
(2008/02/04)
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