| Synthesis and Biological Evaluation of Pyranone Analogues of Territrem B |
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| 作者姓名： | Xiang Rui JIANG Lei AO Chang Xin ZHOU Lei Xiang YANG Hai Bo LI Xiu Mei WU Hua BAI Qi Jun ZHANG Yu ZHAO |
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| 作者单位： | Xiang Rui JIANG1，Lei AO1，Chang Xin ZHOU1，Lei Xiang YANG1，Hai Bo LI1，Xiu Mei WU2，Hua BAI2，Qi Jun ZHANG1，Yu ZHAO11 Department of Traditional Chinese Medicine and Natural Drug Research，College of Pharmaceutical Sciences，Zhejiang University，Hangzhou 310031 2 Zhejiang Hisun Naturelite Pharmaceutical R&D Co.，Ltd.，Hangzhou 310006 |
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| 摘 要： | As a highly selective and potent acetylcholinesterase(AChE)inhibitor,territrem B wasisolated by Ling et al.from a strain of Aspergillus terreus in19791,2.Zhao et alreported mimic preparation of territrem B analogues from triterpenoids and found thatthe enone moiety and aromatic ring played important roles in their syntheticcompounds3,4.To further detect essential pharmacophors for AChE inhibitors,wesimplified the A/B ring system of territrem B and synthesized a number of pyranonepharmacop…
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| 关 键 词： | 吡喃酮 合成方法 2H-吡喃 AChE 生物评价 |
Synthesis and Biological Evaluation of Pyranone Analogues of Territrem B |
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| Xiang Rui JIANG,Lei AO,Chang Xin ZHOU,Lei Xiang YANG,Hai Bo LI,Xiu Mei WU,Hua BAI,Qi Jun ZHANG,Yu ZHAO.Synthesis and Biological Evaluation of Pyranone Analogues of Territrem B[J].Chinese Chemical Letters,2005,16(9):1189-1192. |
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| Authors: | Xiang Rui JIANG Lei AO Chang Xin ZHOU Lei Xiang YANG Hai Bo LI Xiu Mei WU Hua BAI Qi Jun ZHANG Yu ZHAO |
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| Abstract: | 23 compounds containing pyranone pharmacophore of territrem B were designed and synthesized. Some of the analogues showed IC50 values of AChE inhibition at 10-5 mol/L. |
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| Keywords: | 2H-Pyran-2-one territrim B synthesis AChE inhibitor |
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