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4-烃基脲取代Neu5Ac2en衍生物的合成筛选

Synthesis and anti-influenza activity detection of 4-alkylcarbamido substituted Neu5Ac2en derivatives
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摘要 目的合成若干4-烃基脲Neu5Ac2en衍生物并检测其抗病毒活性。方法以5-乙酰氨基-4β-氨基-7,8,9-三-O-乙酰基-2,3,4,5-四脱氧-D-甘油-D-半乳糖-壬-2-烯吡喃糖酸甲酯为起始原料,经过2步反应得到目标化合物,并对目标化合物进行抗病毒活性测定。结果目标化合物的结构均经过核磁共振、质谱确证。结论Neu5Ac2en的4-位被烃基脲替代后失去抗病毒活性。 Objective To synthesize alkylcarbamido substituted Neu5Ac2en derivatives and detect antiinfluenza activity of them. Method The target compounds were prepared by a 2-step process using 5-aeetamido- 4-amino-7, 8, 9-tri-O-aeetyl-2, 3, 4, 5-tetradeoxy-D-galaeto-non-2-enonie acid methyl ester as starting material, their anti-influenza activity were evaluated. Result The structures of all the synthesized compounds were verified by ^1H-NMR and MS. Conclusion All the 4-alkylcarbamido substituted Neu5Ac2en derivatives have no anti-influenza activity under the testing concentration.
出处 《中国抗生素杂志》 CAS CSCD 北大核心 2006年第8期466-470,共5页 Chinese Journal of Antibiotics
基金 国家自然科学基金资助项目(30371674)
关键词 神经氨酸酶 流感病毒 Neu5Ac2en 脲基取代 Neuraminidase Influenza virus Neu5Ac2en Carbamido substituted
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  • 1Calfee D P, Hayden F G. New approaches to influenza chemotherapy[J]. Drugs, 1998, 56(4): 537
  • 2Takeshi H, Takeshi M, Shuku Y, et al. Synthesis and antiinfluenza virus activity of 4-guanidino-7-substituted Neu5Ac2en derivatives[J]. Bioorg Med Chem Lett, 2002, 12:1921
  • 3Takeshi H, Takeshi M, Shuku Y, et al. Synthesis and antiinfluenza virus activity of 7-O-alkylated derivatives related to zamamivir[J]. Bioorg Med Chem Lett, 2002, 12:1925
  • 4Takeshi M, Satoshi S, Masami A, et al. Synthesis and antiinfluenza evaluation of orally active bicyclic ether derivatives related to zamamivir[J]. Bioorg Med Chem Lett, 2003, 13:669
  • 5Varghese J N, Epa V C, Colman P M, et al. Three-dimensional structure of the complex of 4-guanidino-Neu5Ac2en and influenza virus neuraminidase[J]. Protein Sci, 1995, 4:1081
  • 6Von I M, Wu W Y, Kok G B, et al. Rational design of potent sialidase-based inhibitiors of influzena virus replication[J].Nature, 1993, 363:418
  • 7Malcolm C, Mark J B, Richard C, et al. Synthesis of the potent influenza neuraminidase inhibitor 4-guanidino Neu5Ac2en.X-Ray molecular structure of 5-acetamido-4-amino-2,6-anhydro-3, 4, 5-trideoxy -D-erythro-L-gluco-nononicacid [J ].J Chem Soc PerkinTrans, 1995, 1: 1173

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