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Synthesis and Biological Evaluation of Pyranone Analogues of Territrem B
引用本文: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. Synthesis and Biological Evaluation of Pyranone Analogues of Territrem B[J]. 中国化学快报, 2005, 16(9): 1189-1192
作者姓名: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
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
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…

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
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
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
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.
Keywords:2H-Pyran-2-one   territrim B   synthesis   AChE inhibitor.
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