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烟云听雨铁杆木虫 (正式写手)
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[求助]
求翻译一段英文文献（药化）
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In addition to the scaffold bearing the ethyl side chain of stenine and neostenine, a collection of nonnatural Stemonalike ketoamide scaffolds were constructed via this route, which then served as the substrates for the preparation of six sets of functionalized analogues. These bore core changes that could not be readily accomplished by modification of the natural product itself. Representative examples of the various pathways of these initial efforts are shown in Scheme 2. Almost exclusively,these analogues displayed ring systems or functional groups substantially different from those of the natural products, including carbamates, amides, aryl groups, and heterocyclic moieties (e.g., indole and quinoline) (39). At the outset, it was unknown whether these analogues would possess any significant binding activity.We therefore did not feel constrained in the range of chemical manipulations we could explore, and in many cases the final compounds bear little resemblance to any known Stemona alkaloid. Herein, we report the initial evaluation of these compounds against a panel of G protein-coupled receptor (GPCR) targets relevant to central nervous system function and how those results have inspired additional library design, ultimately resulting in a series of highly potent Sig-R ligands. |
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2楼2011-06-28 15:54:15
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