Synthesis and biological evaluation of N-acetylneuraminic acid-based rotavirus inhibitors

Synthesis and biological evaluation of N-acetylneuraminic acid-based rotavirus inhibitors
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DOI:
10.1021/jm950611f
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发表时间:
1996-03-15
影响因子:
7.3
通讯作者:
vonItzstein, M
vonItzstein, M
中科院分区:
医学1区
文献类型:
--
作者:
Kiefel, MJ;Beisner, B;vonItzstein, M

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轮状病毒可引起几种胃肠道疾病,尤其是在婴幼儿中,在第三世界国家尤为普遍。因此,开发该病毒的潜在抑制剂具有重要意义。本研究描述了一些基于N-乙酰神经氨酸的化合物作为潜在的轮状病毒抑制剂的合成和体外生物学评价。我们的数据表明,确实有可能抑制病毒与碳水化合物分子的黏附,从而抑制体外复制,尽管这种抑制似乎与菌株有关。
Rotavirus can cause several gastrointestinal disease, especially in infants and young children, and is particularly prevalent in Third-World countries. Therefore, the development of potential inhibitors of this virus is of great interest. The present study describes the synthesis and in vitro biological evaluation of a number of N-acethyneuraminic acid-based compounds as potential rotavirus inhibitors. Our data suggests that it is indeed possible to inhibit adhesion of the virus, and hence in vitro replication, with carbohydrate-based molecules, although this inhibition, dues appear to be strain dependent.