Comparison of the anti-influenza virus activity of cyclopentane derivatives with oseltamivir and zanamivir in vivo
Comparison of the anti-influenza virus activity of cyclopentane derivatives with oseltamivir and zanamivir in vivo
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DOI：
10.1016/j.bmc.2005.03.048
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发表时间：
2005-06-02
影响因子：
3.5
通讯作者：
Babu, YS
中科院分区：
文献类型：
--
作者：
Chand, P;Bantia, S;Babu, YS
研究了环戊烷衍生物BCX-1812、BCX-1827、BCX-1898和BCX-1923与羧酸奥斯他韦和扎那米韦对感染A/Turkey/Mas/76 X A/Beijing/32/92 （H6N2）流感病毒小鼠的体内活性。以不同剂量水平口服和鼻内测试这些化合物。BCX-1812、BCX-1827和BCX-1923口服剂量为1 mg/kg/天时，保护作用大于50%。即使在0.01 mg/kg/天的剂量下，所有四种化合物的鼻内治疗也100%有效。与羧酸奥司他韦和扎那米韦比较，这四种环戊烷衍生物均表现出相同或更好的疗效。本文还报道了两个新化合物BCX-1898和BCX-1923的合成。(c) 2005 Elsevier Ltd版权所有。
Cyclopentane derivatives, designated as BCX-1812, BCX-1827, BCX-1898, and BCX-1923, were tested in parallel with oseltamivir carboxylate and zanamivir for the in vivo activity in mice infected with A/Turkey/Mas/76 X A/Beijing/32/92 (H6N2) influenza virus. The compounds were tested orally and intranasally at different dose levels. BCX-1812, BCX-1827, and BCX-1923 showed more than 50% protection at 1 mg/kg/day dose level on oral treatment. The intranasal treatment was 100% effective even at 0.01 mg/kg/day for all four compounds. On comparison with oseltamivir carboxylate and zanamivir, these four cyclopentane derivatives have shown equal or better efficacies. The synthesis of two new compounds, BCX-1898 and BCX-1923, is also described. (c) 2005 Elsevier Ltd. All rights reserved.